CN1037514C - 杀真菌原醇的制备方法 - Google Patents

杀真菌原醇的制备方法 Download PDF

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CN1037514C
CN1037514C CN92105930A CN92105930A CN1037514C CN 1037514 C CN1037514 C CN 1037514C CN 92105930 A CN92105930 A CN 92105930A CN 92105930 A CN92105930 A CN 92105930A CN 1037514 C CN1037514 C CN 1037514C
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约翰·科莫
理查德·斯科特·格林伯格
理查德·埃里克·奥尔森
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Abstract

本发明提供了杀真菌的原醇，特别是α-苯乙烯基原醇和相应的环氧原醇及其制备方法。这些原醇或其药物上或农业上合适的盐具有下式结构：
式中E为单链或氧原子，R、R1不为卤素；A、B、Q、R2、R3、R4和n同说明书中定义。

Description

杀真菌原醇的制备方法
本发明是关于杀真菌原醇，特别是关于α-苯乙烯基原醇和相应的环氧原醇的制备方法。
由于持续和广泛地使用免疫抑制治疗，抗微生物治疗和留置导管，系统真菌感染变得越来越严重。当今，在这种真菌感染已有的治疗方面存在着限制。两性霉素B具有任何系统杀真菌药的广谱杀真菌活性，因此仍然是可以选用的药物，但是因其本身的毒性而限制了使用，由于两性霉素B毒性作用的潜在严重性，以及病人在住院治疗期间受这种潜在致命感染，使病人初期治疗时在静脉注射两性霉素B是渐续性。因此，仍然需要开发安全而更有效的药物用于治疗真菌感染。
植物病原真菌和其它疾病的刺激因素也引起每年农作物大量损失。虽然在商业上已有能用于控制许多植物疾病的现有物质，但鉴于需完美的食物和纤维产品，在该领域仍需要进一步改进。
关于吡咯杀真菌药物和植物疾病控制剂方面，有很多的专利和参考文献。同本发明的α-苯乙烯基原醇化合物最密切相关的参考文献如下：
1985年3月26日颁布的美国专利号4,507,140(B.Sugawanam)公开了杀真菌或植物生长调节的β-苯乙烯基三唑或咪唑，其中结构式为：
Figure C9210593000051
式中R1是CH＝CH-X；-C＝C-X或-CH2-CH2-X；X是取代的芳基，芳烷基，或杂环基；R2是烷基，环烷基，或任意取代的芳基；Z是OR3；R3是H，乙酰基；Y是-N-或-CH-。
1980年5月16日公开的德国专利号3,018,865公开了下式的抗真菌剂：
Figure C9210593000061
式中R是烷基，任意取代的环烷基或任意取代的苯基；X是N或一个CH基团；Y是-OCH2-，-CH2CH2-或CH＝CH；Z是卤素，烷基，环烷基，烷氧基，烷硫基等。
1983年4月21日公开的德国专利号3,314,548-A公开了下式取代的1-羟基-乙基-三唑衍生物：式中R是烷基，环烷基成任意取代的苯基；
X是-OCH2-，-SCH2-，-(CH2)p或-CH＝CH-；
Z是卤素，烷基，烷氧基，烷硫基，卤代烷基，卤代烷氧基或卤代烷硫基；
m和p为0，1和2。
这类化合物为抗真菌的，可用于治疗如由念珠菌属，曲霉属菌珠，发癣菌菌珠引起的皮真菌霉菌病和系统霉菌病。
上述三个关于β-苯乙烯基吡咯的参考文献可以认为是最相关的。制备类似于本发明较佳化合物的苯乙烯基吡咯，并发现其几乎不具活性。
1984年8月1日公布的欧洲专利申请114,487号公开了下式的吡咯基乙醇衍生物：
Figure C9210593000071
式中R1和R2可以相同或不同，为氢，烷基，环烷基，烷烯基，杂环芳基或任意取代的芳烷基；W是N或CH；X是C＝O。该化合物具有抗真菌活性和植物生长调节活性。
1984年2月23公布的欧洲专利号117,578-A公开了杂环基-羟基-烷基烷基酮和具下式的类似物：
Figure C9210593000072
式中A是CO；
Q是咪唑基或1H-或4H-1，2，4-三唑-1-基；
R1是H，1-5碳的烷基，或1-8碳的酰基，
R2和R3是1-5碳的烷基，3-6碳的环烷基，
2-6碳的烷烯基，由1-3个卤任意取代的苄基，吡啶基，呋喃基，噻吩基，或由1-3个卤任意取代的苯基，1-3碳的烷基；或1-3碳的烷氧基。
1983年9月22日公布的比利时专利号900,594-A公开了下式的1-苯基-1-吡咯基-羟乙基环烷衍生物。
Figure C9210593000081
式中R1和R2为H，卤素，NO2，低级烷基，烷烯基，烷炔基，烷氧基或烷硫基(由1或多个卤全部任意取代的)，或任意取代的苯基或苯氧基；
R3为H或低级烷基；
R4和R5为H或卤素，
Y为CH或N；
A为2-7碳的烷烯基；
n为0或1。
该化合物是有效的杀真菌剂和抗真菌剂。
这里所引用的参考文献和任何已作的参考文献都没有提到本发明的新颖杀真菌化合物。
按照本发明，提供具有下式的本发明化合物或其药物或农药上合适的盐：
Figure C9210593000082
式中E可为单键或氧原子，规定当其为氧时，RR1不为囟原子；
A是1-8个碳原子的全氟烃基；N(CH3)2
OH；共有1-3个取代基任意取代的萘基(取代基各自为选自卤素和CF3)；1或2个甲基任意取代的共有1-3个取代基任意取代的苯基(该取代基各自选自卤素，1-4个碳原子的烷基，1-4个碳原子的卤代烷基，1-4个碳原子的烷氧基，并且其中不多于一个的基团选自：1-4个碳原子的卤代烷氧基，S(O)mR5，R，2-，3-或4-吡啶基，咪唑-1-基，1，2，4-三唑-1-基，和1或2个甲基任意取代的或选自咪唑-1-基，1，2，4-三唑-1-基，2-或3-噻吩基和任意由1或2个取代基取代的2-，3-，或4-吡啶基的杂环，该每个取代基各选自：卤素，1-4个碳原子的烷基，CF3，和S(O)mR5；
B是1-8个碳原子的烷基，萘基；二苯基；1-8个碳原子的全氟烷基；1-3个取代基任意取代的苯基，每个取代基各选自：卤素，1-4个碳原子的烷基，1-4个碳原子的卤代烷基，1-4个碳原子的烷氧基，并且其中不多于一个的基团是选自1-4个碳原子的卤代烷氧基或S(O)mR5；苯环上由卤素或1-4个碳原子任意取代的苄基或由1或2个甲基在α任意取代的苄基；选自2-或3-噻吩基和由1或2个取代基任意取代的2-，3-，或4-吡啶基的杂环，每个取代基各选自：卤素，1-4个碳原子的烷基，CF3或S(O)mR5；
Q是H，卤素，S(O)mR″，
Figure C9210593000094
，CHO，
Figure C9210593000095
，CO2R13，SCN，SSR12，或SH或其相应的二硫化物，然而当Q不为H时，n为0，R，R1和R4为别为H或CH3，R3为H，并且A和B各为1-3个取代基任意取代的苯基，每个取代基各为卤素，CH3，CF3，OCH3或S(O)mR5；
n为0-4，当A是
Figure C9210593000096
，N(CH3)2或OH时，n不为0；
m每个情况为0，1或2；
X为C，NR10，或O；
R和R1分别是H，1-4个碳原子的烷基，卤素，或苯基，或3-7个碳原子一起组成的环烷基；
R2是H，烯丙基，炔丙基，1-4个碳原子的烷基；
Figure C9210593000101
或含1-4个碳原子的卤代烷基；
R3和R4分别为H，F，或1-4碳原子的烷基；
R5是1-4个碳原子的烷基；
R6是总共有1-3个取代基任意取代的苯基，每个取代基各选自卤素和CF3；
R7是1-4个碳原子的烷基，苯基或苄基；
R8和R9分别为H，1-4个碳原子的烷基，苯基或苄基；
R10为H，1-4个碳原子的烷基，或乙酰基；
R11是1-4个碳原子的烷基，1-4个碳原子的卤代烷基，CH2CN，CH2SCN，CH(CH3)CN，CH2CO2CH3，或CH2CO2CH2CH3；
R12是1-4个碳原子的烷基，烯丙基，1-2个取代基(各为卤素，CH3或OCH3)任意取代的苯基，或1-2个取代基(各为卤素，CH3或OCH3)任意取代的苄基；
R13是H或1-4个碳原子的烷基。
本发明还提供了药物组合物，其包含一种合适的药物载体和治疗有效量的式(I)化合物或其药物上合适的盐，以及使用式(I)化合物为杀真菌剂的方法。
本发明进一步提供了农业组合物，其包含式(I)化合物或其农业上合适的盐及其农业上可接受的稀释剂或载体，以及控制植物的真菌疾病的方法。
本发明的一些化合物可有效用作为除草剂和植物生长调节剂。因此，本发明还关于这些化合物的除草组合物和作为除草剂的使用他们的方法。例如，2-(4-卤代苯基)-3-苯基-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇以2公斤/公顷的施用率可达到90％或更好地控制朝颜花(番薯属菌株)，绒毛叶(_麻属theorhzastis)，crahgrass(马唐属菌株)，giant foxtail)狗毛草属faberii)和稗子(稗属胫-鸡亚目)预育期和crabgyass生育期。
本发明进一步提供制备前述化合物的方法，该方法下文将描述。
另外还提供了下面例子的式(II)和(IIa)新颖的中间体。
Figure C9210593000111
式中A，B，R，R1，R3，R4和n如上定义，但R3，R4不为F和同时不含烷基。
较佳以化合物是式(I)α-苯乙烯基化合物(E是单键)式中：
1，n为0或1；和/或
2，R3和R4分别为H，CH3或F。
较佳化合物中的佳的化合物是：
1，A和B分别为1-3取代基任意取代的苯基，取代基是囟素，1-4个碳原子的烷基，1-4个碳原子的卤代烷基，1-4个碳原子的烷氧基或S(O)mR5；和/或
2，n为0；和/或
3，R和R1各自为H，CH3或卤素；和/或
4，R2为H，1-4个碳原子的烷基，烯丙基或炔丙基；和/或
5，Q是H，I，SH。
较佳化合物中的最佳化合物是：
1，A和B分别为1-3卤原子任意取代的苯基，CH3，OCH3，CF3，或SCH3；和/或
2，R，R1，R2，R3，R4和Q都为H。
下列化合物或其的盐由于他们的生物活性是特别佳的：
(a)2-(4-氟苯基)-3-苯基-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体，
(b)2，3-双(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(c)2-(2，4-二氯苯基)-3-(4-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(d)2-(4-氯苯基)-3-(2-氯苯基)-3-丁烯-2-醇，和其(S)对映体
(e)2-(2，4-二氯苯基)-3-(3-氟苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(f)2-(4-氯苯基)-3-(2-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(g)2-(2，4-二氯苯基)-3-(3-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(h)2-(4-氟苯基)-3-(4-三氟甲基苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(i)2-(2，4-二氯苯基)-3-苯基-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(j)2-(3，4-二氯苯基)-3-(4-氟苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(k)2-(4-二氯苯基)-3-(3-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(l)2-(4-氟苯基)-3-(2，4-二氟苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(m)2-(2，4-氟苯基)-3-(2-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(n)2-(2，4-二氯苯基)-3-苯基-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(o)2-(2，4-二氟苯基)-3-(4-氟苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(p)2-(2-氟苯基)-3-(4-氟苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(q)2-(2-氟苯基)-3-(4-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(r)2-(2，4-二氟苯基)-3-(4-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(s)2-(2-氯苯基)-3-(4-氯苯基)-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
(t)2-(4-氯苯基)-3-苯基-1-(1H-，1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体。
本发明范围的全体化合物在药物或农业杀真菌测定上具有活性。因此，应该认识到这些化合物并不是如同实例中一些化合物在二种测定上都具有活性。上面所列具体优选化合物中，化合物(a)-(n)或他们的盐有较佳药物用途，化合物(n)-(t)或他们的盐有较佳农业用途。
可用本文描述的反应和技术来制备式(I)的新化合物。反应通常是在一种溶剂中进行，该溶剂要适合于所使用的试剂和物质并适合受作用的转移。在一些例子中，起始物质的官能团需要用在化学文献上报导的标准保护基团来保护，这保护方法是本领域技术人员所悉知的。
在一些情况里，起始物质上的取代基可能同描述的一些方法中所需的某些反应条件不相容。这种要求取代基一致于限制的反应条件，对本领域技术人员是显而易见的，因而可使用所描述的替代方法。
本发明化合物能够含有至少一个手性中心，因此可存在二个各自的异构体或他们的外消旋体混合物。本发明是关于(S)异构体，以及关于含有两个异构体的外消旋体混合物。
当存在一个单手性中心，可通过该化合物同一个手性的强酸(例如取代的樟脑磺酸)在一种合适的溶剂(如乙腈)或混合溶剂(如3/1乙醚—丙酮)中反应而完成拆分。在25℃-100℃之间的温度进行反应，最好采用所用溶剂的回流温度。反应得到2种非对映异构的加成物，它们可由分级结晶来分离。然后在碱性介质(如饱和的NaHCO3，饱和的Na2CO3)中，加成物裂开得解析的产品。
式I化合物(式中E为单键，R2和Q为H并且R3，R4不为F和都不为烷基)可由式(II)的环氧乙烷或式(IIa)的卤代醇，或(II)和(IIa)的混合物同三唑或其碱金属盐(最好为Na+或K+的盐在一种合适溶剂中接触而制得(路线I)。
                        路线1X为I，Br，Cl；M为H，碱金属，
当采用三唑时，反应混合物中需加入一种酸接受体，如碳酸钾，甲醇钠或氢化钠。合适的惰性溶剂包括极性的，质子惰性溶剂如二甲基甲酰胺(DMF)，二甲亚砜(DMSO)和醚溶剂如四氢呋喃(THF)如果加入相转移催化剂如四丁基溴化铵的话，可以使用非极性溶剂如甲苯。在10℃至150℃的温度范围，最佳从50℃至120℃进行此反应0.25至24小时。可以看到上述反应中可以得到各种量的式(I)4H-1，2，4-三唑-4-基异构体。如需要的话，可使用标准的拆分技术如色谱来拆分异构体。
按下面一个和两个方法可制备式(II)的环氧乙烷：(路线2)。首先，在醚溶剂如THF或乙醚存在下，温度从-90℃至60℃，最好从-10℃至50℃范围里，通式(III)乙烯基金属有机试剂如乙烯基格氏试剂同通式(IV)卤代酮反应0.5至24小时。根据氏应条件和起始原料(IV)卤代酮的X价数，所得产品可以是环氧乙烷(II)，卤代醇(IIa)或(II)和(IIa)的混合物。如需要的话，可以在如THF溶剂中，同碱如氢化钾(KH)处理卤代醇(IIa)使其转化成环氧乙烷(II)。
                           路线2
Figure C9210593000151
在这第2种方法里，通式(V)的酮一环氧乙烷经烯化作用如用维梯希试剂得到式(II)的环氧一烯烃。
不饱和的式(VII)酮用二甲基、亚甲基硫处理转化成式(II)的环氧一稀烃。式(VI)酮用羰基化合物和合适的催化剂处理可制得enones(VII)(路线)
                路线3
Figure C9210593000161
可使用碱性的过氧化氢使式(VIII)的不饱和酮转化成环氧酮(V)。如前描述，(V)经烯化作用得环氧烯烃(II)(路线4)。
                路线4
Figure C9210593000162
式(III)的乙烯基有机金属化合物可使用标准工艺规程由相应的氯化物，溴化物或碘化物来制备。卤代烯烃，式(IV)卤代酮，式(V)酮一环氧乙烷和式(VI)酮都是已知物可以用本领域技术人员熟知的方法进行制备。
式(I)化合物也可由如线梯希试剂烯化酮(IX)进行制备(路线5)。式中R2，R3和R4为H的(IX)酮是已知的(欧洲专利号117578A)。
                        路线5
通式(I)化合物(式中R3和/或R4不为H)和路线6所示由通式(X)酮同合适的有机金属化合物试剂(例如格氏试剂，有机金属锂试剂)反应制得，而酮(X)可按常规方法从相应的α-卤代酮(IV)制得(参见如欧洲专利号0044605，英国专利2099818A，146224，欧洲专利1337718和0153803)。
                         路线6
可用上述的方法从合适的取代前体制备A为(杂环)-苯基的式(I)化合物或由A为卤代苯基进行取代反应制得。例如在有钯催化剂存在下，用合适的吡啶基锡烷处理A为溴代苯基或碘代苯基的式(I)得到A为(吡啶基)苯基的式(I)化合物(参见四面体通讯27，4407，1986)。借于卤素取代的铜(四面体，40，1433，1984)经杂环亲核试剂提供A例如为1-咪唑基苯基的式(I)化合物。
在一些例子中，希望以A为氨基苯基的式I化合物为起始物，并且使用X(CH2CH2Cl)2构成杂环(见ES8603-473-A)。
按路线7制备Q≠H的式(I)化合物，用强碱金属化(I)(Q＝H)得5-金属化三唑(Ia)(见杂环，23，1645-49，1985)。当R2是H时，需2当量碱。典型的条件包括在THF中于-70℃用正丁基锂处理(I)溶液15-30分钟。在金属化三唑(Ia)对(I)为几乎不溶液的情况下，加入助溶剂如二甲基丙烯脲(DMPV)是有益的。
                          路线7
(Ia)用亲电试剂处理得到Q≠H的各种(I)，本发明所关于的亲电试剂包括卤化剂，硫，二硫化物，二氧化碳，二甲基甲酰胺和二氧化硫以及卤化烷基。采用本领域技术人员所知的方法，经官能作用得到Q≠H的其它式(I)化合物。例如，分别用异氰酸酯或苯二甲酰亚氨基硫化物处理(其中Q为SH)得硫代氨基甲酸盐
Figure C9210593000191
或二硫化物(I；Q＝SSR12)。
E为氧的通式(I)化合物可采用文献中描述的方法(路线8)氧化E是一个单键，并且R和R1不为囟素的式(I)化合物来制备：
                         路线8
Figure C9210593000192
按照取代基的属性，影响氧化反应的合适试剂包括过酸如氯过苯甲酸；在适当的催化剂如丙酮基丙酮酸钒存在下，氢过氧化物如叔丁基氢过氧化物；或过氧化氢。因此，该变化是这样进行的，首先同次卤酸如次溴酸形成一个卤代醇，然后这中间体卤代醇同质子接受体如叔丁氧基钾反应。
本领域技术人员将会看到，根据需氧化的化合物属性，可以获得非对映异构体的混合物。因此这可以通过选择适当的氧化方法来加以控制，或者用常规的方式(如色谱法，分线结晶)来分离所得非对映异构体的混合物。
R2为H的式(I)化合物可以用标准工艺规程进行烷基化，乙酰化和甲氨酰化制备得到其醇部分的官能衍生物。
通过下面的实例可进一步了解本发明的化合物和其制备，但其并不限制本发明。除另有规定以外，这些实例中的所有温度是摄氏度，部分和百分比皆为重量。
除另有指明外，是用CDCl3溶液获得的核磁共振(nmr)光谱，nmr光谱的缩略语S＝单峰，d＝二重峰，t＝三重峰，q＝四重峰，m＝多重峰；峰位是三甲基硅烷中ppm低磁场的部分。
               实例1部分A：2-(4-氟苯基)-2-〔1-(4-氟苯基)乙烯基〕环氧乙烷步骤1：格氏试剂加α-卤代酮
在25℃的格氏试剂〔由6.0克(0.030摩尔)的1-溴-4′-氟苯乙烯和0.85克(0.035摩尔)的镁制成〕的60毫升THF溶液里，加入5.2克(0.030摩尔)2-氯-4′-氟代乙酰苯的10毫升THF溶液。溶液在25℃搅拌2小时。加入饱和的NH4Cl(10毫升)，水相用1∶1的Et2O/己烷萃取，合并有机层，并用盐水洗涤和MgSO4干燥，经蒸发得10.2克琥珀色油。NMR(CDCl3)分析指出，所期望的环氧乙烷为主要产物：δ3.1，3.3(两个d，环氧化物质子)；5.5，5.8(两个S，乙烯基质子)。该物质为足够纯度可用于下步反应。步骤2：2-(4-氟苯基)-2-(4-氟苯甲酰基)环氧乙烷
在冷却至-70℃的4.3克(0.012摩尔)甲基三苯基溴化鏻的15毫升THF的悬浮液中，保持温度不低于-55℃的操作温度时；于3分钟加入8.4毫升(0.013摩尔)的克分子浓度正丁基锂。于10分钟把所得黄色悬浮液加热至0℃，然后用2.6克(0.010摩尔)2-(4-氟苯基)-2-(4-氟苯甲酰基)环氧乙烷的5毫升THF溶液处理。在25℃搅拌这浅棕色悬浮液6小时。经标准表面清洁得3.4克粗产品，再经色谱层析(Et2O)得1.7克的所需产品，这已达足够纯度可供下步使用。NMR(CDCl3)δ3.1(d)；3.3(d)； 5.5(s)；5.8(s)。部分B：2，3-双(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇。
10.2克(0.030摩尔)粗2-(4-氟苯基)-2-〔1-(4-氟苯基)乙烯基〕环氧乙烷和7.0克(0.065摩尔)三唑钾的60毫升DMF的混合液于60℃加热过液，然后冷却并注入100毫升1∶1的Et2O/己烷。有机相经H2O洗三次和盐水洗涤一次后，有机相中形成沉淀物。过滤得4.8克棕色固体，用500毫升环己烷重结晶得2.5克浅褐色粉末，熔点136-137℃：NMR(CDCl3)δ1.7(宽S，OH)；4.7(q，2H)；5.3(S，1H)；5.5(S，1H)；6.8-7.1(m，6H)；7.4(m，2H)；7.8(S，1H)；7.9(S，1H)；IR(液体石蜡)3120(宽)，1900，1600，1505，1220，1139，835厘米-1。
表I中所列化合物已用上述方法制备或可以制得。
在表中，Ph是指苯基和取代的芳基的缩写，例如，4-F-Ph是4-氟苯基，2，4-Cl-Ph是2，4-二氯苯基以及2-噻吩基是指噻吩-2-基。
                               表1实例号         A       B           n  R  R1 R2 R3 R4    熔点℃
1       4-F-Ph   4-F-Ph        0  H  H   H   H   H      136-137
                                                        (HCl盐
                                                        182-184
2       4-F-Ph   2，4-Cl2-Ph  0  H  H   H   H   H      139-143
3       4-F-Ph   4-Cl-Ph       0  H  H   H   H   H      (油)a
4       4-F-Ph   2，4-F2-Ph   0  H  H   H   H   H      102-103.5
5       4-F-Ph   4-CF3-Ph     0  H  H   H   H   H
6       4-F-Ph   n-C4H9      0  H  H   H   H   H      72-73
7       4-F-Ph   n-C4F9      0  H  H   H   H   H
8       2-F-Ph   Ph            0  H  H   H   H   H
9       2-F-Ph   2-F-Ph        0  H  H   H   H   H      89-93
10      2-F-Ph   4-F-Ph        0  H  H   H   H   H      (油)b
11      2-F-Ph   2，4-F2-Ph   0  H  H   H   H   H      121-122
12      2-F-Ph   2-Cl-Ph       0  H  H   H   H   H
13      2-F-Ph   4-Cl-Ph       0  H  H   H   H   H       116-117
14      2-F-Ph   2，4-Cl2-Ph  0  H  H   H   H   H       115-116
15      3-F-Ph   4-F-Ph        0  H  H   H   H   H       106-109
16      3-F-Ph   2，4-Cl2-Ph  0  H  H   H   H   H       145-147
17      3-F-Ph   4-Cl-Ph       0  H  H   H   H   H       101-102
18      3-F-Ph   2，4-F2-Ph   0  H  H   H   H   H
19      3-F-Ph   4-CF3-Ph     0  H  H   H   H   H
20      3-F-Ph   n-C4H9      0  H  H   H   H   H
                         表I(续)实例号     A        B              n  R  R1 R2 R3 R4 熔点℃21    3-F-Ph     n-C4F9       0  H  H    H   H   H22    3-F-Ph     Ph              0  H  H    H   H   H23    3-F-Ph     2-F-Ph          0  H  H    H   H   H24    3-F-Ph     2-Cl-Ph         0  H  H    H   H   H25    4-Cl-Ph    4-F-Ph          0  H  H    H   H   H  110-11526    4-Cl-Ph    2，4-Cl2-Ph    0  H  H    H   H   H  89-91
                                                     (HCl盐
                                                     184-190)27    4-Cl-Ph    4-Cl-Ph         0  H  H    H   H   H  132-13528    4-Cl-Ph    2，4-F2-Ph     0  H  H    H   H   H  124-125.529    4-Cl-Ph    4-CF3-Ph       0  H  H    H   H   H30    4-Cl-Ph    n-C4H9        0  H  H    H   H   H31    4-Cl-Ph    n-C4F9        0  H  H    H   H   H32    2-Cl-Ph    4-F-Ph           0  H  H    H   H   H  (oil)c33    2-Cl-Ph    2，4-Cl2-Ph     0  H  H    H   H   H  150-15234    2-Cl-Ph    4-Cl-Ph          0  H  H    H   H   H  153-154
                                                      (HCl)盐
                                                      175-180)35    2-Cl-Ph    2，4-F2-Ph     0  H  H    H   H   H   128-129
                                                      (HCl盐
                                                      156-161)36    2-Cl-Ph    4-CF3-Ph       0  H  H    H   H   H37    2-Cl-Ph    n-C4H9        0  H  H    H   H   H38    2-Cl-Ph    n-C4F9        0  H  H    H   H   H39    3-Cl-Ph    4-F-Ph           0  H  H    H   H   H   95-96.540    3-Cl-Ph    2，4-Cl2-Ph     0  H  H    H   H   H   144-14641    3-Cl-Ph    4-Cl-Ph          0  H  H    H   H   H   112-115
               表I(续)实例号     A        B          n   R   R1  R2 R3  R4 熔点℃42     3-Cl-Ph   2，4-F2-Ph  0   H   H    H    H    H   115-11643     3-Cl-Ph   -CF3-Ph     0   H   H    H    H    H44     3-Cl-Ph   n-C4H9     0   H   H    H    H    H45     3-Cl-Ph   n-C4F9     0   H   H    H    H    H46     3-Cl-Ph   Ph            0   H   H    H    H    H47     3-Cl-Ph   2-F-Ph        0   H   H    H    H    H   91-9348     3-Cl-Ph   2-Cl-Ph       0   H   H    H    H    H49     Ph        4-F-Ph        0   H   H    H    H    H   125-12650     Ph        2，4-Cl2-Ph  0   H   H    H    H    H   117-12051     Ph        4-Cl-Ph       0   H   H    H    H    H   11152     Ph        2，4-F2-Ph   0   H   H    H    H    H   119.5-122
                                                       (HCl盐
                                                       152-154)53     Ph        4-CF3-Ph     0   H   H    H    H    H54     Ph        n-C4H9      0   H   H    H    H    H55     Ph        n-C4F9      0   H   H    H    H    H56     2-CF3-Ph Ph            0   H   H    H    H    H57     2-CF3-Ph 2-F-Ph        0   H   H    H    H    H58     2-CF3-Ph 2-Cl-Ph       0   H   H    H    H    H59     3-CF3-Ph Ph            0   H   H    H    H    H60     3-CF3-Ph 2-F-Ph        0   H   H    H    H    H61     3-CF3-Ph 2-Cl-Ph       0   H   H    H    H    H62     4-CF3-Ph Ph            0   H   H    H    H    H63     4-CF3-Ph 2-F-Ph        0   H   H    H    H    H64     4-CF3-Ph 2-Cl-Ph       0   H   H    H    H    H
            表I(续)实例号     A           B            n   R   R1  R2  R3  R4 熔点℃65    4-CF3-Ph    4-F-Ph         0   H   H    H    H    H   152-15466    4-CF3-Ph    2，4-Cl2-Ph   0   H   H    H    H    H67    4-CF3-Ph    4-Cl-P  h      0   H   H    H    H    H   144-14568    4-CF3-Ph    2，4-F2-Ph    0   H   H    H    H    H69    4-CF3-Ph    4-CF3-Ph      0   H   H    H    H    H70    4-CF3-Ph    n-C4H9       0   H   H    H    H    H71    4-CF3-Ph    n-C4F9       0   H   H    H    H    H72    2-Br-Ph      Ph              0   H   H    H    H    H73    2-Br-Ph      2-F-Ph          0   H   H    H    H    H74    2-Br-Ph      4-F-Ph          0   H   H    H    H    H75    2-Br-Ph      2，4-F2-Ph     0   H   H    H    H    H76    2-Br-Ph      2-Cl-Ph         0   H   H    H    H    H77    2-Br-Ph      4-Cl-Ph         0   H   H    H    H    H78    2-Br-Ph      2，4-Cl2-Ph    0   H   H    H    H    H79    3-Br-Ph      Ph              0   H   H    H    H    H80    3-Br-Ph      2-F-Ph          0   H   H    H    H    H81    3-Br-Ph      2-Cl-Ph         0   H   H    H    H    H82    4-Br-Ph      Ph              0   H   H    H    H    H83    4-Br-Ph      2-F-Ph          0   H   H    H    H    H84    4-Br-Ph      2-Cl-Ph         0   H   H    H    H    H85    4-Br-Ph      4-F-Ph          0   H   H    H    H    H    (油)d86    4-Br-Ph      2，4-Cl2-Ph    0   H   H    H    H    H87    4-Br-Ph      4-Cl-Ph         0   H   H    H    H    H88    4-Br-Ph      2，4-F2-Ph     0   H   H    H    H    H89    4-Br-Ph      4-CF3-Ph       0   H   H    H    H    H90    4-Br-Ph      n-C4H9        0   H   H    H    H    H
      表I(续)实例号     A             B             n   R   R1 R2  R3  R4 熔点℃91      4-Br-Ph        n-C4F9       0   H   H    H    H    H92      2，4-F2-Ph    Ph             0   H   H    H    H    H93      2，4-F2-Ph    2-F-Ph         0   H   H    H    H    H   106-10894      2，4-F2-Ph    4-F-Ph         0   H   H    H    H    H   100-10395      2，4-F2-Ph    2，4-F2-Ph    0   H   H    H    H    H   116-12096      2，4-F2-Ph    2-Cl-Ph        0   H   H    H    H    H97      2，4-F2-Ph    4-Cl-Ph        0   H   H    H    H    H98      2，4-F2-Ph    2，4-Cl2-Ph   0   H   H    H    H    H99      2，4-Cl2-Ph   4-F-Ph         0   H   H    H    H    H   (油)e100     2，4-Cl2-Ph   2，4-Cl2-Ph   0   H   H    H    H    H   75-78101     2，4-Cl2-Ph   4-Cl-Ph        0   H   H    H    H    H   60-62102     2，4-Cl2-Ph   2，4-F2-Ph    0   H   H    H    H    H   106-109103     2，4-Cl2-Ph   4-CF3-Ph      0   H   H    H    H    H104     2，4-Cl2-Ph   n-C4H9       0   H   H    H    H    H105     2，4-Cl2-Ph   n-C4F9       0   H   H    H    H    H106     2，4-Cl2-Ph   Ph              0   H   H    H    H    H107     2，4-Cl2-Ph   2-F-Ph          0   H   H    H    H    H   68-73108     2，4-Cl2-Ph   2-Cl-Ph         0   H   H    H    H    H109     3，4-Cl2-Ph   Ph              0   H   H    H    H    H110     3，4-Cl2-Ph   2-F-Ph          0   H   H    H    H    H111     3，4-Cl2-Ph   2-Cl-Ph         0   H   H    H    H    H112     4-t-Bu-Ph      Ph              0   H   H    H    H    H113     4-t-Bu-Ph      2-F-Ph          0   H   H    H    H    H
             表I(续)实例号     A               B          n   R   R1 R2 R3 R4  熔点℃114   4-t-Bu-Ph       4-F-Ph        0   H   H   H    H   H    110-113115   4-t-Bu-Ph       2，4-F2-Ph   0   H   H   H    H   H116   4-t-Bu-Ph       2-Cl-Ph       0   H   H   H    H   H117   4-t-Bu-Ph       4-Cl-Ph       0   H   H   H    H   H    (油)f118   4-t-Bu-Ph       2，4-Cl2-Ph  0   H   H   H    H   H119   2-CH3S-Ph      Ph            0   H   H   H    H   H120   2-CH3S-Ph      2-F-Ph        0   H   H   H    H   H121   2-CH3S-Ph      4-F-Ph        0   H   H   H    H   H122   2-CH3S-Ph      2，4-F2-Ph   0   H   H   H    H   H123   2-CH3S-Ph      2-Cl-Ph       0   H   H   H    H   H124   2-CH3S-Ph      4-Cl-Ph       0   H   H   H    H   H125   2-CH3S-Ph      2，4-Cl2-Ph  0   H   H   H    H   H126   2-CH3S(O)-Ph   Ph            0   H   H   H    H   H127   2-CH3S(O)-Ph   2-F-Ph        0   H   H   H    H   H128   2-CH3S(O)-Ph   4-F-Ph        0   H   H   H    H   H129   2-CH3S(O)-Ph   2，4-F2-Ph   0   H   H   H    H   H130   2-CH3S(O)-Ph   2-Cl-Ph       0   H   H   H    H   H131   2-CH3S(O)-Ph   4-Cl-Ph       0   H   H   H    H   H132   2-CH3S(O)-Ph   2，4-Cl2-Ph  0   H   H   H    H   H133   2-CH3S(O)2-Ph Ph            0   H   H   H    H   H134   2-CH3S(O)2-Ph 2-F-Ph        0   H   H   H    H   H135   2-CH3S(O)2-Ph 4-F-Ph        0   H   H   H    H   H136   2-CH3S(O)2-Ph 2，4-F2-Ph   0   H   H   H    H   H
              表I(续)实例号     A                B          n   R   R1  R2  R3  R4  熔点℃137   2-CH3S(O)2-Ph   2-Cl-Ph       0   H   H    H    H    H138   2-CH3S(O)2-Ph   4-Cl-Ph       0   H   H    H    H    H139   2-CH3S(O)2-Ph   2，4-Cl2-Ph  0   H   H    H    H    H140   3-CH3S-Ph        Ph             0   H   H    H    H    H141   3-CH3S-Ph        2-F-Ph         0   H   H    H    H    H142   3-CH3S-Ph        4-F-Ph         0   H   H    H    H    H143   3-CH3S-Ph        2，4-F2-Ph    0   H   H    H    H    H144   3-CH3S-Ph        2-Cl-Ph        0   H   H    H    H    H145   3-CH3S-Ph        4-Cl-Ph        0   H   H    H    H    H146   3-CH3S-Ph        2，4-Cl2-Ph   0   H   H    H    H    H147   3-CH3S(O)-Ph     Ph             0   H   H    H    H    H148   3-CH3S(O)-Ph     2-F-Ph         0   H   H    H    H    H149   3-CH3S(O)-Ph     4-F-Ph         0   H   H    H    H    H150   3-CH3S(O)-Ph     2，4-F2-Ph    0   H   H    H    H    H151   3-CH3S(O)-Ph     2-Cl-Ph        0   H   H    H    H    H152   3-CH3S(O)-Ph     4-Cl-Ph        0   H   H    H    H    H153   3-CH3S(O)-Ph     2，4-Cl2-Ph   0   H   H    H    H    H154   3-CH3S(O)2-Ph   Ph             0   H   H    H    H    H155   3-CH3S(O)2-Ph   2-F-Ph         0   H   H    H    H    H156   3-CH3S(O)2-Ph   4-F-Ph         0   H   H    H    H    H157   3-CH3S(O)2-Ph   2，4-F2-Ph    0   H   H    H    H    H158   3-CH3S(O)2-Ph   2-Cl-Ph        0   H   H    H    H    H159   3-CH3S(O)2-Ph   4-Cl-Ph        0   H   H    H    H    H160   3-CH3S(O)2-Ph   2，4-Cl2-Ph   0   H   H    H    H    H
              表I(续)实例号      A              B           n   R   R1  R2 R3  R4  熔点℃161    4-CH3S-Ph      Ph             0   H   H    H    H    H162    4-CH3S-Ph      2-F-Ph         0   H   H    H    H    H163    4-CH3S-Ph      4-F-Ph         0   H   H    H    H    H   140-142164    4-CH3S-Ph      2，4-F2-Ph    0   H   H    H    H    H   81-83165    4-CH3S-Ph      2-Cl-Ph        0   H   H    H    H    H166    4-CH3S-Ph      4-Cl-Ph        0   H   H    H    H    H167    4-CH3S-Ph      2，4-Cl2-Ph   0   H   H    H    H    H168    4-CH3S(O)-Ph   Ph             0   H   H    H    H    H169    4-CH3S(O)-Ph   2-F-Ph         0   H   H    H    H    H170    4-CH3S(O)-Ph   4-F-Ph         0   H   H    H    H    H   81-84171    4-CH3S(O)-Ph   2，4-F2-Ph    0   H   H    H    H    H   131-134172    4-CH3S(O)-Ph   2-Cl-Ph        0   H   H    H    H    H173    4-CH3S(O)-Ph   4-Cl-Ph        0   H   H    H    H    H174    4-CH3S(O)-Ph   2，4-Cl2-Ph   0   H   H    H    H    H175    4-CH3S(O)2-Ph Ph             0   H   H    H    H    H176    4-CH3S(O)2-Ph 2-F-Ph         0   H   H    H    H    H177    4-CH3S(O)2-Ph 4-F-Ph         0   H   H    H    H    H   135178    4-CH3S(O)2-Ph 2，4-F2-Ph    0   H   H    H    H    H179    4-CH3S(O)2-Ph 2-Cl-Ph        0   H   H    H    H    H180    4-CH3S(O)2-Ph 4-Cl-Ph        0   H   H    H    H    H181    4-CH3S(O)2-Ph 2，4-Cl2-Ph   0   H   H    H    H    H
          表I(续)实例号     A               B          n   R   R1  R2 R3  R4   熔点℃182   3-n-BuS(O)-Ph    4-F-Ph       0   H   H    H    H    H183   3-n-BuS(O)-Ph    2，4-F2-Ph  0   H   H    H    H    H184   3-n-BuS(O)-Ph    4-Cl-Ph      0   H   H    H    H    H185   3-n-BuS(O)-Ph    2-4-Cl2-Ph  0   H   H    H    H    H186   2-CF3O-Ph       Ph           0   H   H    H    H    H187   2-CF3O-Ph       2-F-Ph       0   H   H    H    H    H188   2-CF3O-Ph       4-F-Ph       0   H   H    H    H    H189   2-CF3O-Ph       2，4-F2-Ph  0   H   H    H    H    H190   2-CF3O-Ph       2-Cl-Ph      0   H   H    H    H    H191   2-CF3O-Ph       4-Cl-Ph      0   H   H    H    H    H192   2-CF3O-Ph       2，4-Cl2-Ph 0   H   H    H    H    H193   3-CF3O-Ph       Ph           0   H   H    H    H    H194   3-CF3O-Ph       2-F-Ph       0   H   H    H    H    H195   3-CF3O-Ph       4-F-Ph       0   H   H    H    H    H196   3-CF3O-Ph       2，4-F2-Ph  0   H   H    H    H    H197   3-CF3O-Ph       2-Cl-Ph      0   H   H    H    H    H198   3-CF3O-Ph       4-Cl-Ph      0   H   H    H    H    H199   3-CF3O-Ph       2，4-Cl2-Ph 0   H   H    H    H    H200   4-CF3O-Ph       Ph           0   H   H    H    H    H201   4-CF3O-Ph       2-F-Ph       0   H   H    H    H    H202   4-CF3O-Ph       4-F-Ph       0   H   H    H    H    H203   4-CF3O-Ph       2，4-F2-Ph  0   H   H    H    H    H204   4-CF3O-Ph       2-Cl-Ph      0   H   H    H    H    H
      表I(续)实例号      A           B           n   R   R1 R2  R3  R4 熔点℃205    4-CF3O-Ph    4-Cl-Ph      0   H   H    H    H    H206    4-CF3O-Ph    2，4-Cl2-Ph 0   H   H    H    H    H207    4-F-1-萘基    2-F-Ph        0   H   H    H    H    H208    1-萘基        4-F-Ph        0   H   H    H    H    H   104-106209    1-″″        2，4-F2-Ph   0   H   H    H    H    H210    1-″″        2-Cl-Ph       0   H   H    H    H    H211    2-Cl-1-萘基   4-Cl-Ph       0   H   H    H    H    H212    1-萘基        2，4-Cl2-Ph  0   H   H    H    H    H213    2-″″        2-F-Ph        0   H   H    H    H    H214    2-″″        4-F-Ph        0   H   H    H    H    H215    2-″″        2，4-F2-Ph   0   H   H    H    H    H216    2-″″        2-Cl          0   H   H    H    H    H217    1-Cl-2-萘基   4-Cl-Ph       0   H   H    H    H    H218    2-萘基        2，4-Cl2-Ph  0   H   H    H    H    H219    2-噻吩基      Ph            0   H   H    H    H    H220    2-″″″      2-F-Ph        0   H   H    H    H    H221    2-″″″      4-F-Ph        0   H   H    H    H    H222    2-″″″      2，4-F2-Ph   0   H   H    H    H    H223    2-″″″      2-Cl-Ph       0   H   H    H    H    H224    2-″″″      4-Cl-Ph       0   H   H    H    H    H225    2-″″″      2，4-Cl2-Ph  0   H   H    H    H    H226    3-″″″      Ph            0   H   H    H    H    H227    3-″″″      2-F-Ph        0   H   H    H    H    H228    3-″″″      4-F-Ph        0   H   H    H    H    H229    3-″″″      2，4-F2-Ph   0   H   H    H    H    H230    3-″″″      2-Cl-Ph       0   H   H    H    H    H231    3-″″″      4-Cl-Ph       0   H   H    H    H    H232    3-″″″      2，4-Cl2-Ph  0   H   H    H    H    H
           表I(续)实例号      A                B            n   R  R1  R2  R3  R4熔点℃233     2-Cl-3-噻吩基       Ph           0   H   H    H    H    H234     2-Cl-3-″″″       2-F-Ph       0   H   H    H    H    H235     2-Cl-3-″″″       2-Cl-Ph      0   H   H    H    H    H236     5-Cl-2-″″″       Ph           0   H   H    H    H    H237     5-Cl-2-″″″       2-F-Ph       0   H   H    H    H    H238     5-Cl-2-″″″       2-Cl-Ph      0   H   H    H    H    H239     2，5-Cl2-3-噻吩基  Ph           0   H   H    H    H    H240     2，5-Cl2-3-″″″  2-F-Ph       0   H   H    H    H    H241     2，5-Cl2-3-″″″  4-F-Ph       0   H   H    H    H    H242     2，5-Cl2-3-″″″  2，4-F2-Ph  0   H   H    H    H    H243     2，5-Cl2-3-″″″  2-Cl-Ph      0   H   H    H    H    H244     2，5-Cl2-3-″″″  4-Cl-Ph      0   H   H    H    H    H245     2，5-Cl2-3-″″″  2，4-Cl2-Ph 0   H   H    H    H    H246     5-溴-2-噻吩基       Ph            0   H   H    H    H    H247     5-″ ″ ″″″      2-F-Ph        0   H   H    H    H    H248     5-″ ″ ″″″      4-F-Ph        0   H   H    H    H    H249     5-″ ″ ″″″      2，4-F2-Ph   0   H   H    H    H    H250     5-″ ″ ″″″      2-Cl-Ph       0   H   H    H    H    H251     5-″ ″ ″″″      4-Cl-Ph       0   H   H    H    H    H252     5-″ ″ ″″″      2，4-Cl2-Ph  0   H   H′  H    H    H253     2-吡啶基            Ph            0   H   H    H    H    H254     2-″″″            2-F-Ph        0   H   H    H    H    H255     2-″″″            2-Cl-Ph       0   H   H    H    H    H256     3-″″″            Ph            0   H   H    H    H    H257     3-″″″            2-F-Ph        0   H   H    H    H    H258     3-″″″            2-Cl-Ph       0   H   H    H    H    H
      表I(续)实例号      A          B              n   R   R1 R2  R3  R4熔点℃259    4-吡啶基       Ph             0   H   H    H    H    H260    4-″″″       2-F-Ph         0   H   H    H    H    H261    4-″″″       2-Cl-Ph        0   H   H    H    H    H262    5-Cl-2-吡啶基  Ph             0   H   H    H    H    H263    5-Cl-2-″″″  2-F-Ph         0   H   H    H    H    H264    5-Cl-2-″″″  2-Cl-Ph        0   H   H    H    H    H265    2-Cl-3-″″″  Ph             0   H   H    H    H    H266    2-Cl-3-″″″  2-F-Ph         0   H   H    H    H    H267    2-Cl-3-″″″  4-F-Ph         0   H   H    H    H    H268    2-Cl-3-″″″  2，4-F2-Ph    0   H   H    H    H    H269    2-Cl-3-″″″  2-Cl-Ph        0   H   H    H    H    H270    2-Cl-3-″″″  4-Cl-Ph        0   H   H    H    H    H271    2-Cl-3-″″″  2，4-Cl2-Ph   0   H   H    H    H    H272    3-Cl-2-″″″  Ph             0   H   H    H    H    H273    3-Cl-2-″″″  2-F-Ph         0   H   H    H    H    H274    3-Cl-2-″″″  4-F-Ph         0   H   H    H    H    H275    3-Cl-2-″″″  2，4-F2-Ph    0   H   H    H    H    H276    3-Cl-2-″″″  2-Cl-Ph        0   H   H    H    H    H277    3-Cl-2-″″″  4-Cl-Ph        0   H   H    H    H    H278    3-Cl-2-″″″  2，4-Cl2-Ph   0   H   H    H    H    H279    6-Cl-3-″″″  Ph             0   H   H    H    H    H280    6-Cl-3-″″″  2-F-Ph         0   H   H    H    H    H281    6-Cl-3-″″″  4-F-Ph         0   H   H    H    H    H282    6-Cl-3-″″″  2，4-F2-Ph    0   H   H    H    H    H283    6-Cl-3-″″″  2-Cl-Ph        0   H   H    H    H    H284    6-Cl-3-″″″  4-Cl-Ph        0   H   H    H    H    H285    6-Cl-3-″″″  2，4-Cl2-Ph   0   H   H    H    H    H
             表I(续)实例号 Ar         B         n   R     R1   R2  R3  R4 熔点℃286   Ph      4-F-Ph       0   H     CH3  H    H    H   108-111287   Ph      4-F-Ph       0   H     F     H    H    H288   Ph      4-F-Ph       0   H     Cl    H    H    H289   Ph      4-F-Ph       0   H     Br    H    H    H290   Ph      4-F-Ph       0  -(CH2)2-  H    H    H291   Ph      4-F-Ph       0   H     Ph    H    H    H    (油)g292   Ph      4-F-Ph       0   CH3  CH3 H    H    H293   Ph      4-F-Ph       0   F     F     H    H    H294   Ph      4-F-Ph       0   Cl    Cl    H    H    H295   4-F-Ph  4-F-Ph       0   H     CH3  H    H    H296   4-F-Ph  4-F-Ph       0   H     F     H    H    H297   4-F-Ph  4-F-Ph       0   H     Cl    H    H    H298   4-F-Ph  4-F-Ph       0   H     Br    H    H    H299   4-F-Ph  4-F-Ph       0  -(CH2)2-  H    H    H300   4-F-Ph  4-F-Ph       0   CH3  CH3 H    H    H301   4-F-Ph  4-F-Ph       0   F     F     H    H    H302   4-F-Ph  4-F-Ph       0   Cl    Cl    H    H    H303   4-Cl-Ph 2，4-Cl2-Ph 0   H     CH3  H    H    H304   4-Cl-Ph 2，4-Cl2-Ph 0   H     F     H    H    H305   4-Cl-Ph 2，4-Cl2-Ph 0   H     Cl    H    H    H306   4-Cl-Ph 2，4-Cl2-Ph 0   H     Br    H    H    H307   4-Cl-Ph 2，4-Cl2-Ph 0  -(CH2)2-  H    H    H308   4-Cl-Ph 2，4-Cl2-Ph 0   CH3  CH3 H    H    H309   4-Cl-Ph 2，4-Cl2-Ph 0   F     F     H    H    H310   4-Cl-Ph 2，4-Cl2-Ph 0   Cl    Cl    H    H    H311   2-Cl-Ph 4-Cl-Ph      0   H     CH3  H    H    H312   2-Cl-Ph 4-Cl-Ph      0   H     F     H    H    H
         表I(续)实例号  A          B       n   R      R1      R2  R3 R4  熔点℃313 2-Cl-Ph    4-Cl-Ph    0   H      Cl        H    H    H314 2-Cl-Ph    4-Cl-Ph    0   H      Br        H    H    H315 2-Cl-Ph    4-Cl-Ph    0   -(CH2)2-      H    H    H316 2-Cl-Ph    4-Cl-Ph    0   CH3   CH3     H    H    H317 2-Cl-Ph    4-Cl-Ph    0   F      F         H    H    H318 2-Cl-Ph    4-Cl-Ph    0   Cl     Cl        H    H    H319 4-F-Ph     4-F-Ph     0   H      C2H5   H    H    H320 4-F-Ph     4-F-Ph     0   H      i-C3H7 H    H    H321 4-F-Ph     4-F-Ph     0   H      n-C4H9 H    H    H322 4-F-Ph     4-F-Ph     0   H      Ph        H    H    H323 4-F-Ph     4-F-Ph     0   CH3   t-C4H9 H    H    H324 4-F-Ph     4-F-Ph     0   CH3   Ph        H    H    H325 4-F-Ph     4-F-Ph     0   H      I         H    H    H326 4-F-Ph     4-F-Ph     0   CH3   F         H    H    H327 4-F-Ph     4-F-Ph     0   CH3   Cl        H    H    H328 4-F-Ph     4-F-Ph     0   Br     Br         H    H    H329 4-F-Ph     4-F-Ph     0  -(CH2)3-        H    H    H330 4-F-Ph     4-F-Ph     0  -(CH2)4-        H    H    H331 4-F-Ph     4-F-Ph     0  -(CH2)5-        H    H    H332 4-F-Ph     4-F-Ph     0  -(CH2)6-        H    H    H333 4-CH3-Ph  4-F-Ph     0   H      CH3      H    H    H334 4-F-Ph     4-F-Ph     1   H      CH3      H    H    H335 4-Cl-Ph    4-F-Ph     4   H      CH3      H    H    H336 n-C4F9   4-F-Ph     0   H      CH3     H    H    H337 (CH3)2N  4-F-Ph     1   H      CH3     H    H    H338 5-Cl-thio-  4-F-Ph     0   H      CH3     H    H    H
phen-2-yl
    表I(续)实例号   A             B       n   R     R1  R2  R3  R4  熔点℃339 2-Cl-噻吩      4-F-Ph     0   H    CH3  H    H    H
     -3-基340 1-咪唑基       4-F-Ph     0   H    CH3  H    H    H341 1，2，4-三唑   4-F-Ph     0   H    CH3  H    H    H
 1-基342 5-C1-2-        4-F-Ph     0   H    CH3  H    H    H
 -吡啶基343 4-F-Ph         n-C4H9   0   H    CH3  H    H    H344 4-F-Ph         t-C4H9   0   H    CH3  H    H    H345 4-F-Ph         n-C4F9   0   H    CH3  H    H    H346 4-CH3-Ph      4-F-Ph     0   H     F     H    H    H347 4-F-Ph         4-F-Ph     1   H     F     H    H    H348 4-Cl-Ph        4-F-Ph     4   H     F     H    H    H349 n-C4F9      4-F-Ph      0   H    F     H    H    H350 (CH3)2N     4-F-Ph      1   H    F     H    H    H351 5-Cl-          4-F-Ph      0   H    F     H    H    H
 噻吩-
 -2-基352 2-Cl-          4-F-Ph      0   H    F     H    H    H
 噻吩
 2-基353 1-咪唑基       4-F-Ph      0   H    F     H    H    H354 1，2，4-       4-F-Ph      0   H    F     H    H    H
 三唑-1-
 1-基355 5-Cl-2-        4-F-Ph      0   H    F     H    H    H
 -吡啶基356 4-F-Ph         n-C4H9    0   H    F     H    H    H357 4-F-Ph         t-C4H9    0   H    F     H    H    H358 4-F-Ph         n-C4F9    0   H    F     H    H    H
                   表I(续)实例号  A       B           n   R   R1   R2         R3  R4  熔点℃359 4-F-Ph  4-F-Ph         0   H   H     CH3         H    H   (油)h360 4-F-Ph  4-F-Ph         0   H   H     CH2CH＝CH2 H    H   (油)i361 4-F-Ph  4-F-Ph         0   H   H     COCH3       H    H   (油)j362 4-F-Ph  4-F-Ph         0   H   H     CO2CH3     H    H363 4-F-Ph  4-F-Ph         0   H   H     CONHCH3     H    H   164-167364 4-F-Ph  4-F-Ph         0   H   H     CONH-nBu     H    H365 4-F-Ph  4-F-Ph         0   H   H     CONHPh       H    H366 4-F-Ph  4-F-Ph         0   H   H     CONH-        H    H
                                      (4-F-Ph)367 4-F-Ph  4-F-Ph         0   H   H     CON(CH3)2  H    H368 2-Cl-Ph 4-Cl-Ph        0   H   H     CH3         H    H369 2-Cl-Ph 4-Cl-Ph        0   H   H     CH2CH＝CH2 H    H370 2-Cl-Ph 4-Cl-Ph        0   H   H     COCN3       H    H371 2-Cl-Ph 4-Cl-Ph        0   H   H     CO2CH3     H    H372 2-Cl-Ph 4-Cl-Ph        0   H   H     CONHCH3     H    H373 2-Cl-Ph 4-Cl-Ph        0   H   H     CONH-nBu     H    H374 2-Cl-Ph 4-Cl-Ph        0   H   H     CONHPh       H    H375 2-Cl-Ph 4-Cl-Ph        0   H   H     CONH-        H    H
                                     (4-F-Ph)376 2-Cl-Ph 4-Cl-Ph       0   H   H      CON(CH3)2  H    H377 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      CH3         H    H378 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      CH2CH＝CH2 H    H379 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      COCH3       H    H380 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      CO2CH3     H    H381 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      CONHCH3     H    H382 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      CONH-nBu     H    H383 4-Cl-Ph 2，4-Cl2-Ph  0   H   H      CONHPh       H    H
            表I(续)实例号 A          B          n   R   R1   R2          R3 R4熔点℃384 4-Cl-Ph  2，4-Cl2-Ph   0   H   H   CONH(4-F-Ph)   H    H385 4-Cl-Ph  2，4-Cl2-Ph   0   H   H   CON(CH3)2    H    H386 Ph       4-F-Ph         0   H   H   CH3           H    H387 Ph       4-F-Ph         0   H   H   CH2CH＝CH2   H    H388 Ph       4-F-Ph         0   H   H   COCH3         H    H389 Ph       4-F-Ph         0   H   H   CO2CH3       H    H390 Ph       4-F-Ph         0   H   H   CONHCH3       H    H391 Ph       4-F-Ph         0   H   H   CONH-nBu        H    H392 Ph       4-F-Ph         0   H   H   CONHPh          H    H393 Ph       4-F-Ph         0   H   H   CONH(4-F-Ph)    H    H394 Ph       4-F-Ph         0   H   H   CON(CH3)2    H    H395 4-F-Ph   4-F-Ph         0   H   H   C2H5         H    H396 4-F-Ph   4-F-Ph         0   H   H   i-C3H7       H    H397 4-F-Ph   4-F-Ph         0   H   H   n-C4CH9      H    H398 4-F-Ph   4-F-Ph         0   H   H   COC2H5       H    H399 4-F-Ph   4-F-Ph         0   H   H   CO-tC4H9     H    H400 4-F-Ph   4-F-Ph         0   H   H   COPh            H    H401 4-F-Ph   4-F-Ph         0   H   H   COCH2Ph        H    H402 4-F-Ph   4-F-Ph         0   H   H   CONH2          H    H403 4-F-Ph   4-F-Ph         0   H   H   CONH-iC3H7    H    H404 4-F-Ph   4-F-Ph         0   H   H   CONHCH2Ph      H    H405 4-F-Ph   4-F-Ph         0   H   H   CON(CH3)Ph     H    H
             表I(续)实例号 A       B          n   R   R1    R2              R3 R4熔点℃406 4-F-Ph  4-F-Ph       0   H   H    CONH(4-Cl-Ph)       H   H407 4-F-Ph  4-F-Ph       0   H   H    CONH(4-CH3-Ph)     H   H408 4-F-Ph  4-F-Ph       0   H   H    CONH(4-CH3-Ph)     H   H409 4-F-Ph  4-F-Ph       0   H   H    CONH(3-CF3-Ph)     H   H410 4-F-Ph  4-F-Ph       0   H   H    CONH(4-NO2-Ph)     H   H411 4-F-Ph  4-F-Ph       0   H   H    CONH(2-CH3-Ph)     H   H412 4-F-Ph  4-F-Ph       0   H   H    CONH(2，4-F2-Ph)   H   H413 4-F-Ph  4-F-Ph       0   H   H    CONH(2，4-Cl2-Ph)  H   H414 4-F-Ph  4-F-Ph       0   H   H    CO2C2H5          H   H415 4-F-Ph  4-F-Ph       0   H   H    CO2-nC4H9        H   H416 4-F-Ph  4-F-Ph       0   H   H    CO2-tC4H9        H   H417 4-F-Ph  4-F-Ph       0   H   H    CO2CH2Ph          H   H418 4-F-Ph  4-F-Ph       0   H   H    CO2Ph              H   H419 4-F-Ph  4-F-Ph       0   H   H    CF2H               H   H420 4-F-Ph  4-F-Ph       0   H   H    CH2CF3            H   H421 4-F-Ph  4-F-Ph       0   H   H    CH2CH2CH2F       H   H422 4-F-Ph  4-F-Ph       0   H   H    CH2CH2CH2CH2Cl  H   H423 Ph      2，4-F2-Ph  0   H   H    CH2-C≡CH           H   H424 Ph      4-Cl-Ph      0   H   H    CH2-C≡CH           H   H425 4-F-Ph  2-F-Ph       0   H   H    CH2-C≡CH           H   H426 4-F-Ph  4-F-Ph       0   H   H    CH2-C≡CH           H   H427 4-F-Ph  2，4-F2-Ph  0   H   H    CH2-C≡CH           H   H428 4-F-Ph  2-Cl-Ph      0   H   H    CH2-C≡CH           H   H429 2-Cl-Ph 2，4-F2-Ph  0   H   H    CH2-C≡CH           H   H
                      表I(续)实例号  A         B            n   R  R1 R2         R3 R4熔点℃430 2-Cl-Ph   4-Cl-Ph         0   H   H  CH2-C≡CH   H   H431 4-Cl-Ph   2-F-Ph          0   H   H  CH2-C≡CH   H   H432 4-Cl-Ph   2，4-F2-Ph     0   H   H  CH2-C≡CH   H   H433 4-F-Ph    4-F-Ph          1   H   H   H            H   H434 4-F-Ph    4-F-Ph          2   H   H   H            H   H435 4-F-Ph    4-F-Ph          3   H   H   H            H   H436 4-F-Ph    4-F-Ph          4   H   H   H            H   H437 2-Cl-Ph   4-Cl-Ph         1   H   H   H            H   H438 2-Cl-Ph   4-Cl-Ph         2   H   H   H            H   H439 2-Cl-Ph   4-Cl-Ph         3   H   H   H            H   H440 2-Cl-Ph   4-Cl-Ph         4   H   H   H            H   H441 4-Cl-Ph   2，4-Cl2-Ph    1   H   H   H            H   H
               表I(续)实例号  A          B            n   R   R1 R2 R3  R4  熔点℃442 4-Cl-Ph     2，4-Cl2-Ph    2   H   H   H    H    H443 4-Cl-Ph     2，4-Cl2-Ph   3   H   H   H    H    H444 4-Cl-Ph     2，4-Cl2-Ph   4   H   H   H    H    H445 Ph          4-F-Ph         1   H   H   H    H    H446 Ph          4-F-Ph         2   H   H   H    H    H447 OH          4-Cl-Ph        1   H   H   H    H    H    (油)k448 OH          Ph             1   H   H   H    H    H    94-100449 OH          2，4-Cl2-Ph   1   H   H   H    H    H    166-168450 OH          4-F-Ph         1   H   H   H    H    H    115-116451 OH          4-Br-Ph        1   H   H   H    H    H    (foam)452 OH          4-Ph-Ph        1   H   H   H    H    H    140-143453 (CH3)2N   2，4-Cl2-Ph  1   H   H   H    H    H    104-107454 (CH3)2N   4-F-Ph        1   H   H   H    H    H    (油)m455 (CH3)2N   4-Br-Ph       1   H   H   H    H    H    (″)n456 (CH3)2N   4-Ph-Ph       1   H   H   H    H    H    (″)o457 1-咪唑基     4-F-Ph        1   H   H   H    H    H458 1-″″″     4-F-Ph        2   H   H   H    H    H459 1-″″″     4-F-Ph        3   H   H   H    H    H460 1-″″″     4-F-Ph        4   H   H   H    H    H461 1H-1，2，4-  4-F-Ph        1   H   H   H    H    H
  三唑-1-基462 ″           4-F-Ph        2   H   H   H    H    H463 ″           4-F-Ph        3   H   H   H    H    H464 ″           4-F-Ph        4   H   H   H    H    H465 ″           2，4-Cl2-Ph  1   H   H   H    H    H466 ″           2，4-Cl2-Ph  2   H   H   H    H    H
              表I(续)实例号A                         B           n   R   R1 R2 R3  R4 熔点℃467 1-咪唑基                 2，4-Cl2-Ph   1   H   H   H    H    H468 1-哌啶基                 Ph             1   H   H   H    H    H469 1-″″″                 2-F-Ph         1   H   H   H    H    H470 1-″″″                 4-F-Ph         1   H   H   H    H    H471 1-″″″                 2，4-F2-Ph    1   H   H   H    H    H472 1-″″″                 2-Cl-Ph        1   H   H   H    H    H473 1-″″″                 4-Cl-Ph        1   H   H   H    H    H474 1-″″″                 2，4-Cl2-Ph   1   H   H   H    H    H475 2，6-(CH3)2-1-吗啉基  Ph              1   H   H   H    H    H476 2，6-(CH3)2-1-″″″  2-F-Ph          1   H   H   H    H    H477 2，6-(CH3)2-1-″″″  4-F-Ph          1   H   H   H    H    H   97-99478 2，6-(CH3)2-1-″″″  2，4-F2-Ph     1   H   H   H    H    H479 2，6-(CH3)2-1-″″″  2-Cl-Ph         1   H   H   H    H    H480 2，6-(CH3)2-1-″″″  4-Cl-Ph         1   H   H   H    H    H481 2，6-(CH3)2-1-″″″  2，4-Cl2-Ph    1   H   H   H    H    H482 4-CH3-1-哌嗪基         Ph               1   H   H   H    H    H483 4-CH3-1-″″″         2-F-Ph           1   H   H   H    H    H484 4-CH3-1-″″″         4-F-Ph           1   H   H   H    H    H485 4-CH3-1-″″″         2，4-F2-Ph      1   H   H   H    H    H486 4-CH3-1-″″″         2-Cl-Ph          1   H   H   H    H    H487 4-CH3-1-″″″         4-Cl-Ph          1   H   H   H    H    H488 4-CH3-1-″″″         2，4-Cl2-Ph     1   H   H   H    H    H489 4-n-Bu-1-″″″         Ph                1   H   H   H    H    H490 4-n-Bu-1-″″″         2-F-Ph            1   H   H   H    H    H
             表I(续)实例号 A                           B          n  R  R1 R2 R3 R4491 4-n-Bu-1-哌嗪基             4-F-Ph       1  H  H   H    H   H492 4-n-Bu-1-″″″             2，4-F2-Ph  1  H  H   H    H   H493 4-n-Bu-1-″″″             2-Cl-Ph      1  H  H   H    H   H494 4-n-Bu-1-″″″             4-Cl-Ph      1  H  H   H    H   H495 4-n-Bu-1-″″″             2，4-Cl2-Ph 1  H  H   H    H   H496 4-乙酰基-1-哌嗪基           Ph           1  H  H   H    H   H497 4-″″″″ ″″″           2-F-Ph       1  H  H   H    H   H498 4-″″″″ ″″″           4-F-Ph       1  H  H   H    H   H499 4-″″″″ ″″″           2，4-F2-Ph  1  H  H   H    H   H500 4-″″″″ ″″″           2-Cl-Ph      1  H  H   H    H   H501 4-″″″″ ″″″           4-Cl-Ph      1  H  H   H    H   H502 4-″″″″ ″″″           2，4-Cl2-Ph 1  H  H   H    H   H503 2-(2-吡啶基)-Ph             4-F-Ph       0  H  H   H    H   H504 2-(3-″″″)-Ph             4-F-Ph       0  H  H   H    H   H505 2-(4-″″″)-Ph             4-F-Ph       0  H  H   H    H   H506 3-(2-″″″)-Ph             4-F-Ph       0  H  H   H    H   H507 3-(3-″″″)-Ph             4-F-Ph       0  H  H   H    H   H508 3-(4-″″″)-Ph             4-F-Ph       0  H  H   H    H   H509 4-(2-″″″)-Ph             4-F-Ph       0  H  H   H    H   H510 4-(3-″″″)-Ph             4-F-Ph       0  H  H   H    H   H511 4-(4-″″″)-Ph             4-F-Ph       0  H  H   H    H   H512 2-(1H-1，2，4-三唑-1-基)-Ph 4-F-Ph       0  H  H   H    H   H513 3-(1H-1，2，4-         )-Ph 4-F-Ph       0  H  H   H    H   H514 4-(1H-1，2，4-         )-Ph 4-F-Ph       0  H  H   H    H   H515 2-(咪唑-1-基)-Ph            4-F-Ph       0  H  H   H    H   H516 3-(″″″ ″)-Ph            4-F-Ph       0  H  H   H    H   H517 4-(″″″ ″)-Ph            4-F-Ph       0  H  H   H    H   H518 2-(4-甲基哌嗪-1-基)-Ph      4-F-Ph       0  H  H   H    H   H
            表I(续)实例号  A                         B          n   R   R1 R2 R3 R4519 3-(4-甲基哌嗪-1-基)-Ph      4-F-Ph      0   H   H    H   H   H520 4-(4-″″″″ ″″)-Ph      4-F-Ph      0   H   H    H   H   H521 2-(4-乙酰基哌嗪-1-基)-Ph    4-F-Ph      0   H   H    H   H   H522 3-(4-″″″″″ ″″)-Ph    4-F-Ph      0   H   H    H   H   H523 4-(4-″″″″″ ″″)-Ph    4-F-Ph      0   H   H    H   H   H524 2-(2-吡啶基)-Ph             2，4-F2-Ph 0   H   H    H   H   H525 2-(3-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H526 2-(4-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H527 3-(2-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H528 3-(3-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H529 3-(4-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H530 4-(2-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H531 4-(3-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H532 4-(4-″″″)-Ph             2，4-F2-Ph 0   H   H    H   H   H533 2-(1H-1，2，4-三唑-1-基)-Ph 2，4-F2-Ph 0   H   H    H   H   H534 3-(1H-1，2，4-″   ″″)-Ph 2，4-F2-Ph 0   H   H    H   H   H535 4-(1H-1，2，4-″   ″″)-Ph 2，4-F2-Ph 0   H   H    H   H   H536 2-(咪唑-1-基)-Ph            2，4-F2-Ph 0   H   H    H   H   H537 3-( ″ ″ ″)-Ph            2，4-F2-Ph 0   H   H    H   H   H538 4-( ″ ″ ″)-Ph            2，4-F2-Ph 0   H   H    H   H   H539 2-(4-甲基哌嗪-2-基)-Ph      2，4-F2-Ph 0   H   H    H   H   H540 3-(4-″  ″  ″ ″)-Ph      2，4-F2-Ph 0   H   H    H   H   H541 4-(4-″  ″  ″ ″)-Ph      2，4-F2-Ph 0   H   H    H   H   H
                表I(续)实例号 A              B             B          n   R   R1 R2 R3 R4542 2-(4-乙酰基哌嗪-1-基)-Ph    2，4-F2-Ph   0   H   H    H   H   H543 3-(4-″″″     ″″)-Ph    2，4-F2-Ph   0   H   H    H   H   H544 4-(4-″″″     ″″)-Ph    2，4-F2-Ph   0   H   H    H   H   H545 2-Cl-3-(3-吡啶基)-Ph        2，4-F2-Ph   0   H   H    H   H   H546 2-(2-吡啶基)-Ph             4-Cl-Ph       0   H   H    H   H   H547 2-(3-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H548 2-(4-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H549 3-(2-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H550 3-(3-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H551 3-(4-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H552 4-(2-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H553 4-(3-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H554 4-(4-″″″)-Ph             4-Cl-Ph       0   H   H    H   H   H555 2-(1H-1，2，4-三唑-1-基)-Ph 4-Cl-Ph       0   H   H    H   H   H556 3-(1H-1，2，4-″   ″″)-Ph 4-Cl-Ph       0   H   H    H   H   H557 4-(1H-1，2，4-″   ″″)-Ph 4-Cl-Ph       0   H   H    H   H   H558 2-(咪唑-1-基)-Ph            4-Cl-Ph       0   H   H    H   H   H559 3-(″   ″″)-Ph            4-Cl-Ph       0   H   H    H   H   H560 4-(″   ″″)-Ph            4-Cl-Ph       0   H   H    H   H   H561 2-(4-甲基哌嗪-1-基)-Ph      4-Cl-Ph       0   H   H    H   H   H562 3-(4-″″     ″″)-Ph      4-Cl-Ph       0   H   H    H   H   H563 4-(4-″″     ″″)-Ph      4-Cl-Ph       0   H   H    H   H   H564 2-(4-″″     ″″)-Ph      4-Cl-Ph       0   H   H    H   H   H565 3-(4-″″     ″″)-Ph      4-Cl-Ph       0   H   H    H   H   H566 4-(4-″″     ″″)-Ph      4-Cl-Ph       0   H   H    H   H   H567 2-Cl-3-(3-吡啶基)-Ph        4-Cl-Ph       0   H   H    H   H   H568 2-(2-吡啶基)-Ph             2，4-Cl2-Ph  0   H   H    H   H   H569 2-(3-″″″)-Ph             2，4-Cl2-Ph  0   H   H    H   H   H570 2-(4-″″″)-Ph             2，4-Cl2-Ph  0   H   H    H   H   H
                  表I(续)实例号   A                          B        n   R   R1  R2  R3 R4571 3-(2-吡啶基)-Ph             2，4-Cl2-Ph 0   H   H    H    H    H572 3-(3-″″″)-Ph             2，4-Cl2-Ph 0   H   H    H    H    H573 3-(4-″″″)-Ph             2，4-Cl2-Ph 0   H   H    H    H    H574 4-(2-″″″)-Ph             2，4-Cl2-Ph 0   H   H    H    H    H575 4-(3-″″″)-Ph             2，4-Cl2-Ph 0   H   H    H    H    H576 4-(4-″″″)-Ph             2，4-Cl2-Ph 0   H   H    H    H    H577 2-(1H-1，2，4-三唑-1-基)-Ph 2，4-Cl2-Ph 0   H   H    H    H    H578 3-(1H-1，2，4-″   ″″)-Ph 2，4-Cl2-Ph 0   H   H    H    H    H579 4-(1H-1，2，4-″   ″″)-Ph 2，4-Cl2-Ph 0   H   H    H    H    H580 2-(咪唑-1-基)-Ph            2，4-Cl2-Ph 0   H   H    H    H    H581 3-(″   ″″)-Ph            2，4-Cl2-Ph 0   H   H    H    H    H582 4-(″   ″″)-Ph            2，4-Cl2-Ph 0   H   H    H    H    H583 2-(4-甲基哌嗪-1-基)-Ph      2，4-Cl2-Ph 0   H   H    H    H    H584 3-(4-″  ″   ″″)-Ph      2，4-Cl2-Ph 0   H   H    H    H    H585 4-(4-″  ″   ″″)-Ph      2，4-Cl2-Ph 0   H   H    H    H    H586 2-(4-乙酰基-哌嗪-1-基)-Ph   2，4-Cl2-Ph 0   H   H    H    H    H587 3-(4-″″″ ″   ″″)-Ph   2，4-Cl2-Ph 0   H   H    H    H    H588 4-(4-″″″ ″   ″″)-Ph   2，4-Cl2-Ph 0   H   H    H    H    H589 2-Cl-3-(3-吡啶基)-Ph        2，4-Cl2-Ph 0   H   H    H    H    H590 3-(吗啉-1-基)-Ph            2，4-F2-Ph  0   H   H    H    H    H591 3-(二甲基-吗啉-1-基         2，4-F2-Ph  0   H   H    H    H    H592 4-(n-丁基-哌嗪-1-基)-Ph     2，4-F2-Ph  0   H   H    H    H    H593 4-(哌啶-1-基)-Ph            2，4-F2-Ph  0   H   H    H    H    H
               表I(续)实例号A      B             n   R   R1  R2 R3  R4 熔点℃594 Ph    2-F-Ph           0   H   H    H    H    H   (油)p
                                                  (HCl盐
                                                  190-195)595 Ph    3-F-Ph           0   H   H    H    H    H596 Ph    2-Cl-Ph          0   H   H    H    H    H   78-80597 Ph    3-Cl-Ph          0   H   H    H    H    H598 Ph    4-Br-Ph          0   H   H    H    H    H   92-95599 Ph    4-I-Ph           0   H   H    H    H    H600 Ph    3，4-F2-Ph      0   H   H    H    H    H601 Ph    3，4-Cl2-Ph     0   H   H    H    H    H602 Ph    2，6-Cl2-Ph     0   H   H    H    H    H603 Ph    3，5-Cl2-Ph     0   H   H    H    H    H   142-144604 Ph    2-Cl-(4-F)-Ph    0   H   H    H    H    H605 Ph    3-Cl-(4-F)-Ph    0   H   H    H    H    H   119-124
                                                  (dec.)606 Ph    2，4，6-Cl3-Ph  0   H   H    H    H    H607 Ph    2-F-(4-Cl)-Ph    0   H   H    H    H    H608 Ph    Ph               0   H   H    H    H    H   130-133609 Ph    4-CH3-Ph        0   H   H    H    H    H610 Ph    3-CH3-Ph        0   H   H    H    H    H611 Ph    2-CH3-Ph        0   H   H    H    H    H   160.5-163612 Ph    2-CF3-Ph        0   H   H    H    H    H613 Ph    3-CF3-Ph        0   H   H    H    H    H614 Ph    2-Cl-3-噻吩基    0   H   H    H    H    H615 Ph    2-F-(4-CF3)-Ph  0   H   H    H    H    H
              表I(续)实例号A          B             n   R   R1  R2  R3  R4  熔点℃616 Ph       4-CH3O-Ph       0   H   H    H    H    H617 Ph       5-Cl-2-吡啶基    0   H   H    H    H    H618 Ph       5-Cl-2-噻吩基    0   H   H    H    H    H     88-90619 Ph       s-C4H9        0   H   H    H    H    H620 2-Cl-Ph  2-F-Ph           0   H   H    H    H    H     118-119621 2-Cl-Ph  3-F-Ph           0   H   H    H    H    H622 2-Cl-Ph  2-Cl-Ph          0   H   H    H    H    H     149-150623 2-Cl-Ph  3-Cl-Ph          0   H   H    H    H    H624 2-Cl-Ph  4-Br-Ph          0   H   H    H    H    H     151-152625 2-Cl-Ph  4-I-Ph           0   H   H    H    H    H626 2-Cl-Ph  3，4-F2-Ph      0   H   H    H    H    H627 2-Cl-Ph  3，4-Cl2-Ph     0   H   H    H    H    H     122-123.5628 2-Cl-Ph  2，6-Cl2-Ph     0   H   H    H    H    H629 2-Cl-Ph  2-Cl-(4-F)-Ph    0   H   H    H    H    H630 2-Cl-Ph  2，4，6-Cl3-Ph  0   H   H    H    H    H631 2-Cl-Ph  2-F-(4-Cl)-Ph    0   H   H    H    H    H632 2-Cl-Ph  Ph               0   H   H    H    H    H633 2-Cl-Ph  4-CH3-Ph        0   H   H    H    H    H634 2-Cl-Ph  3-CH3-Ph        0   H   H    H    H    H635 2-Cl-Ph  2-CH3-Ph        0   H   H    H    H    H636 2-Cl-Ph  2-CF3-Ph        0   H   H    H    H    H637 2-Cl-Ph  3-CF3-Ph        0   H   H    H    H    H638 2-Cl-Ph  2-F-(4-CF3)-Ph  0   H   H    H    H    H639 2-Cl-Ph  4-CH3O-Ph       0   H   H    H    H    H640 2-Cl-Ph  5-Cl-2-吡啶基    0   H   H    H    H    H
              表I(续)实例号  A         B              n   R   R1  R2 R3  R4 熔点℃641 2-Cl-Ph   5-Cl-2-噻吩基     0   H   H    H    H    H642 2-Cl-Ph   2-Cl-3-″″″     0   H   H    H    H    H643 2-Cl-Ph   s-C4H9         0   H   H    H    H    H644 4-F-Ph    2-F-Ph            0   H   H    H    H    H   96-97645 4-F-Ph    3-F-Ph            0   H   H    H    H    H646 4-F-Ph    2-Cl-Ph           0   H   H    H    H    H   116-119647 4-F-Ph    3-Cl-Ph           0   H   H    H    H    H648 4-F-Ph    4-Br-Ph           0   H   H    H    H    H   114-116649 4-F-Ph    4-I-Ph            0   H   H    H    H    H650 4-F-Ph    3，4-F2-Ph       0   H   H    H    H    H651 4-F-Ph    3，4-Cl2-Ph      0   H   H    H    H    H   98-99652 4-F-Ph    2，6-Cl2-Ph      0   H   H    H    H    H653 4-F-Ph    2-Cl-(4-F)-Ph     0   H   H    H    H    H654 4-F-Ph    2，4，6-Cl3-Ph   0   H   H    H    H    H655 4-F-Ph    2-F-(4-Cl)-Ph     0   H   H    H    H    H656 4-F-Ph    Ph                0   H   H    H    H    H   124-125657 4-F-Ph    4-Ph-Ph           0   H   H    H    H    H   116-119658 4-F-Ph    4-CH3-Ph         0   H   H    H    H    H   145-147659 4-F-Ph    2-CH3-Ph         0   H   H    H    H    H   145-149660 4-F-Ph    2-CF3-Ph         0   H   H    H    H    H661 4-F-Ph    3-CF3-Ph         0   H   H    H    H    H   121-122662 4-F-Ph    2-F-(4-CF3)-Ph   0   H   H    H    H    H663 4-F-Ph    4-CH3O-Ph        0   H   H    H    H    H   112-114664 4-F-Ph    5-Cl-2-吡啶基     0   H   H    H    H    H665 4-F-Ph    5-Cl-2-噻吩基     0   H   H    H    H    H   114-115666 4-F-Ph    2-Cl-3-″″″     0   H   H    H    H    H
            表I(续)实例号 A        B              n   R   R1 R2  R3  R4 熔点℃667 4-F-Ph   i-C3H7        0   H   H    H    H    H   74-75668 4-F-Ph   C2H5          0   H   H    H    H    H   (油)q669 4-Cl-Ph  2-F-Ph           0   H   H    H    H    H   130-131670 4-Cl-Ph  3-F-Ph           0   H   H    H    H    H671 4-Cl-Ph  2-Cl-Ph          0   H   H    H    H    H   137-139672 4-Cl-Ph  3-Cl-Ph          0   H   H    H    H    H673 4-Cl-Ph  4-Br-Ph          0   H   H    H    H    H   121-123674 4-Cl-Ph  4-I-Ph           0   H   H    H    H    H675 4-Cl-Ph  3，4-Cl2-Ph     0   H   H    H    H    H   107-198676 4-Cl-Ph  2，6-Cl2-Ph     0   H   H    H    H    H677 4-Cl-Ph  2-Cl-(4-F)-Ph    0   H   H    H    H    H678 4-Cl-Ph  2，4，6-Cl3-Ph  0   H   H    H    H    H679 4-Cl-Ph  2-F-(4-Cl)-Ph    0   H   H    H    H    H680 4-Cl-Ph  Ph               0   H   H    H    H    H681 4-Cl-Ph  4-CH3-Ph        0   H   H    H    H    H682 4-Cl-Ph  3-CH3-Ph        0   H   H    H    H    H683 4-Cl-Ph  2-CH3-Ph        0   H   H    H    H    H684 4-Cl-Ph  2-CF3-Ph        0   H   H    H    H    H685 4-Cl-Ph  3-CF3-Ph        0   H   H    H    H    H    103-104686 4-Cl-Ph  2-F-(4-CF3)-Ph  0   H   H    H    H    H687 4-Cl-Ph  4-CH3O-Ph       0   H   H    H    H    H688 4-Cl-Ph  5-Cl-2-吡啶基    0   H   H    H    H    H689 4-Cl-Ph  5-Cl-2-噻吩基    0   H   H    H    H    H690 4-Cl-Ph  2-Cl-3-″″″    0   H   H    H    H    H
                     表I(续)实例号 A                    B                n   R   R1  R2 R3  R4 熔点℃691 4-Cl-Ph              s-C4H9          0   H   H    H    H    H692 4-F-Ph                 0   H   H    H    H    H693 4-F-Ph               t-丁基            0   H   H    H    H    H694 4-F-Ph               n-己基            0   H   H    H    H    H695 4-F-Ph               n-庚基            0   H   H    H    H    H696 4-F-Ph               2，4-(CH3)2-Ph 0   H   H    H    H    H   148-149697 4-F-Ph               -C6F13         0   H   H    H    H    H698 4-F-Ph               -C8F17         0   H   H    H    H    H699 4-F-Ph               4-吡啶基         0   H   H    H    H    H    175-178700 4-F-Ph               2-″″″         0   H   H    H    H    H701 4-F-Ph               2-噻吩基         0   H   H    H    H    H702 4-F-Ph               4-n-丁基         0   H   H    H    H    H703 4-F-Ph               4-n-丁氧基苯基   0   H   H    H    H    H704 4-F-Ph               5-CF3-吡啶-2-   0   H   H    H    H    H
                       -基705 4-F-Ph               5-MeSO2-2-      0   H   H    H    H    H
                       -噻吩基706 4-C2H5-Ph          4-F-Ph           0   H   H    H    H    H707 4-(n-BuO)-Ph          4-F-Ph           0   H   H    H    H    H708 2-CH3SO2-          4-F-Ph           0   H   H    H    H    H
 咪唑-1-基709 5-CH3-1，2，4-      4-F-Ph           0   H   H    H    H    H
 三唑-1-基710-C6F13              4-F-Ph           0   H   H    H    H    H711-C8F17              4-F-Ph           0   H   H    H    H    H712 2-Cl-3-(3-吡啶基)-Ph 4-F-Ph           0   H   H    H    H    H
                  表I(续)实例号 A                   B       n   R   R1 R2  R3  R4 熔点℃713 2-CF3-咪唑-1-基    4-F-Ph    0   H   H    H    H    H714 4-(i-丙)-Ph         4-F-Ph    0   H   H    H    H    H715 4-I-Ph              4-F-Ph    0   H   H    H    H    H716 3，4-F2-Ph         4-F-Ph    0   H   H    H    H    H717 3，4-Cl2-Ph        4-F-Ph    0   H   H    H    H    H718 2，6-Cl2-Ph        4-F-Ph    0   H   H    H    H    H719 2-Cl-(4-F)-Ph       4-F-Ph    0   H   H    H    H    H720 2，4，6-Cl3-Ph     4-F-Ph    0   H   H    H    H    H721 4-CH3-Ph           4-F-Ph    0   H   H    H    H    H   119-120722 3-CH3-Ph           4-F-Ph    0   H   H    H    H    H723 2-CH3-Ph           4-F-Ph    0   H   H    H    H    H724 2-CF3-Ph           4-F-Ph    0   H   H    H    H    H   110-112725 3-CF3-Ph           4-F-Ph    0   H   H    H    H    H   106-108726 4-CH3O-Ph          4-F-Ph    0   H   H    H    H    H   109-111727 2，3-Cl2-Ph        4-F-Ph    0   H   H    H    H    H728 3，5-Cl2-Ph        4-F-Ph    0   H   H    H    H    H729 2，5-Cl2-Ph        4-F-Ph    0   H   H    H    H    H730 3-Br-Ph             4-F-Ph    0   H   H    H    H    H731 4-EtO-Ph            4-F-Ph    0   H   H    H    H    H732 2，4-(CH3)2-Ph    4-F-Ph    0   H   H    H    H    H733 2，4，6-(CH3)3-Ph 4-F-Ph    0   H   H    H    H    H734 4-Ph-Ph              4-F-Ph    0   H   H    H    H    H735 5-Cl-2-噻吩基        4-F-Ph    0   H   H    H    H    H736 2-Cl-3-″″″        4-F-Ph    0   H   H    H    H    H
                   表I(续)实例号 A                  B           n   R   R1 R2  R3  R4737 1-咪唑基           4-F-Ph        0   H   H    H    H    H738 1H-1，2，4-三唑基  4-F-Ph        0   H   H    H    H    H739 2-吡啶基           4-F-Ph        0   H   H    H    H    H740 5-Cl-吡啶-2-基     4-F-Ph        0   H   H    H    H    H741 3-吡啶基           4-F-Ph        0   H   H    H    H    H742 4-″″″           4-F-Ph        0   H   H    H    H    H743 n-C4F9          4-F-Ph        0   H   H    H    H    H744 4-I-Ph             2，4-Cl2-Ph 0   H   H    H    H    H745 3，4-F2-Ph        2，4-Cl2-Ph 0   H   H    H    H    H746 3，4-Cl2-Ph       2，4-Cl2-Ph 0   H   H    H    H    H747 2，6-Cl2-Ph       2，4-Cl2-Ph 0   H   H    H    H    H748 2-Cl-(4-F)-Ph      2，4-Cl2-Ph 0   H   H    H    H    H749 2，4，6-Cl3-Ph    2，4-Cl2-Ph 0   H   H    H    H    H750 4-CH3-Ph          2，4-Cl2-Ph 0   H   H    H    H    H751 3-CH3-Ph          2，4-Cl2-Ph 0   H   H    H    H    H752 2-CH3-Ph          2，4-Cl2-Ph 0   H   H    H    H    H753 2-CF3-Ph          2，4-Cl2-Ph 0   H   H    H    H    H754 3-CF3-Ph          2，4-Cl2-Ph 0   H   H    H    H    H755 4-CH3O-Ph         2，4-Cl2-Ph 0   H   H    H    H    H756 2，3-Cl2-Ph       2，4-Cl2-Ph 0   H   H    H    H    H757 3，5-Cl2-Ph       2，4-Cl2-Ph 0   H   H    H    H    H758 2，5-Cl2-Ph       2，4-Cl2-Ph 0   H   H    H    H    H759 3-Br-Ph            2，4-Cl2-Ph 0   H   H    H    H    H760 4-EtO-Ph           2，4-Cl2-Ph 0   H   H    H    H    H
             表I(续)实例号A                       B         n   R   R1  R2  R3 R4761 2，4-(CH3)2-Ph      2，4-Cl2-Ph 0   H   H    H    H    H762 2，4，6-(CH3)3-Ph   2，4-Cl2-Ph 0   H   H    H    H    H763 4-Ph-Ph                2，4-Cl2-Ph 0   H   H    H    H    H764 5-Cl-2-噻吩基          2，4-Cl2-Ph 0   H   H    H    H    H765 2-Cl-3-″″″          2，4-Cl2-Ph 0   H   H    H    H    H766 1-咪唑基               2，4-Cl2-Ph 0   H   H    H    H    H767 1H-1，2，4-三唑-1-基   2，4-Cl2-Ph 0   H   H    H    H    H768 2-吡啶基               2，4-Cl2-Ph 0   H   H    H    H    H769 5-Cl-吡啶-2-基         2，4-Cl2-Ph 0   H   H    H    H    H770 3-吡啶基               2，4-Cl2-Ph 0   H   H    H    H    H771 4-″″″               2，4-Cl2-Ph 0   H   H    H    H    H772 n-C4F9              2，4-Cl2-Ph 0   H   H    H    H    H773 4-I-Ph                 4-Cl-Ph      0   H   H    H    H    H774 3，4-F2-Ph            4-Cl-Ph      0   H   H    H    H    H775 3，4-Cl2-Ph           4-Cl-Ph      0   H   H    H    H    H776 2，6-Cl2-Ph           4-Cl-Ph      0   H   H    H    H    H777 2-Cl-(4-F)-Ph          4-Cl-Ph      0   H   H    H    H    H778 2，4，6-Cl3-Ph        4-Cl-Ph      0   H   H    H    H    H779 4-CH3-Ph              4-Cl-Ph      0   H   H    H    H    H780 3-CH3-Ph              4-Cl-Ph      0   H   H    H    H    H781 2-CH3-Ph              4-Cl-Ph      0   H   H    H    H    H782 2-CF3-Ph              4-Cl-Ph      0   H   H    H    H    H783 3-CF3-Ph              4-Cl-Ph      0   H   H    H    H    H
              表I(续)实例号  A                    B           n  R  R1  R2 R3 R4 熔点℃784 4-CH3O-Ph             4-Cl-Ph      0  H  H    H    H   H785 2，3-Cl2-Ph           4-Cl-Ph      0  H  H    H    H   H786 3，5-Cl2-Ph           4-Cl-Ph      0  H  H    H    H   H787 2，5-Cl2-Ph           4-Cl-Ph      0  H  H    H    H   H788 3-Br-Ph                4-Cl-Ph      0  H  H    H    H   H789 4-EtO-Ph               4-Cl-Ph      0  H  H    H    H   H790 2，4-(CH3)2-Ph      4-Cl-Ph      0  H  H    H    H   H791 2，4，6-(CH3)3-Ph   4-Cl-Ph      0  H  H    H    H   H792 4-Ph-Ph                4-Cl-Ph      0  H  H    H    H   H793 5-Cl-2-噻吩基          4-Cl-Ph      0  H  H    H    H   H794 2-Cl-3-″″″          4-Cl-Ph      0  H  H    H    H   H795 1-咪唑基               4-Cl-Ph      0  H  H    H    H   H796 1H-1，2，4-三唑-1-基1  4-Cl-Ph      0  H  H    H    H   H797 2-吡啶基               4-Cl-Ph      0  H  H    H    H   H798 5-Cl-吡啶-2-基         4-Cl-Ph      0  H  H    H    H   H799 3-吡啶基               4-Cl-Ph      0  H  H    H    H   H800 4-″″″               4-Cl-Ph      0  H  H    H    H   H801 n-C4F9              4-Cl-Ph      0  H  H    H    H   H802 4-I-Ph                 2，4-F2-Ph 0  H  H    H    H   H803 3，4-F2-Ph            2，4-F2-Ph 0  H  H    H    H   H804 3，4-Cl2-Ph           2，4-F2-Ph 0  H  H    H    H   H805 2，6-Cl2-Ph           2，4-F2-Ph 0  H  H    H    H   H806 2-Cl-(4-F)-Ph          2，4-F2-Ph 0  H  H    H    H   H807 2，4，6-Cl3-Ph        2，4-F2-Ph 0  H  H    H    H   H808 4-CH3-Ph              2，4-F2-Ph 0  H  H    H    H   H  129-130.5
              表I(续)实例号 A                          B     n   R R1  R2 R3 R4 熔点℃809 3-CH3-Ph              2，4-F2-Ph 0  H  H    H   H   H810 2-CH3-Ph              2，4-F2-Ph 0  H  H    H   H   H811 2-CF3-Ph              2，4-F2-Ph 0  H  H    H   H   H812 3-CF3-Ph              2，4-F2-Ph 0  H  H    H   H   H813 4-CH3O-Ph             2，4-F2-Ph 0  H  H    H   H   H    88-89814 2，3-Cl2-Ph           2，4-F2-Ph 0  H  H    H   H   H815 3，5-Cl2-Ph           2，4-F2-Ph 0  H  H    H   H   H    173-175816 2，5-Cl2-Ph           2，4-F2-Ph 0  H  H    H   H   H817 3-Br-Ph                2，4-F2-Ph 0  H  H    H   H   H818 4-EtO-Ph               2，4-F2-Ph 0  H  H    H   H   H819 2，4-(CH3)2-Ph      2，4-F2-Ph 0  H  H    H   H   H820 2，4，6-(CH3)3-Ph   2，4-F2-Ph 0  H  H    H   H   H821 4-Ph-Ph                2，4-F2-Ph 0  H  H    H   H   H822 5-Cl-2-噻吩基          2，4-F2-Ph 0  H  H    H   H   H823 2-Cl-3-″″″          2，4-F2-Ph 0  H  H    H   H   H824 1-咪唑基               2，4-F2-Ph 0  H  H    H   H   H825 1H-1，2，4-三唑-1-基   2，4-F2-Ph 0  H  H    H   H   H826 2-pyridyl              2，4-F2-Ph 0  H  H    H   H   H827 5-Cl-吡啶-2-基         2，4-F2-Ph 0  H  H    H   H   H828 3-吡啶基               2，4-F2-Ph 0  H  H    H   H   H829 4-″″″               2，4-F2-Ph 0  H  H    H   H   H830 n-C4F9              2，4-F2-Ph 0  H  H    H   H   H
             表I(续)实例号  A                B       n R   R1 R2 R3 R4熔点℃831  2-F-Ph          4-Br-Ph    0 H   H   H    H   H832  3-F-Ph          4-Br-Ph    0 H   H   H    H   H833  3-Cl-Ph         4-Br-Ph    0 H   H   H    H   H834  4-Br-Ph         4-Br-Ph    0 H   H   H    H   H835  2，4-F2-Ph     4-Br-Ph    0 H   H   H    H   H836  2，4-Cl2-Ph    4-Br-Ph    0 H   H   H    H   H837  2-CF3-Ph       4-Br-Ph    0 H   H   H    H   H838  3-CF3-Ph       4-Br-Ph    0 H   H   H    H   H839  4-CF3-Ph       4-Br-Ph    0 H   H   H    H   H840  2-F-Ph          4-I-Ph     0 H   H   H    H   H841  3-F-Ph          4-I-Ph     0 H   H   H    H   H842  3-Cl-Ph         4-I-Ph     0 H   H   H    H   H843  4-Br-Ph         4-I-Ph     0 H   H   H    H   H844  2，4-F2-Ph     4-I-Ph     0 H   H   H    H   H845  2，4-Cl2-Ph    4-I-Ph     0 H   H   H    H   H846  2-CF3-Ph       4-I-Ph     0 H   H   H    H   H847  3-CF3-Ph       4-I-Ph     0 H   H   H    H   H848  4-CF3-Ph       4-I-Ph     0 H   H   H    H   H849  2-F-Ph          2-CH3-Ph  0 H   H   H    H   H850  3-F-Ph          2-CH3-Ph  0 H   H   H    H   H851  3-Cl-Ph         2-CH3-Ph  0 H   H   H    H   H852  4-Br-Ph         2-CH3-Ph  0 H   H   H    H   H853  2，4-F2-Ph     2-CH3-Ph  0 H   H   H    H   H854  2，4-Cl2-Ph    2-CH3-Ph  0 H   H   H    H   H
            表I(续)实例号   A                  B         n R  R1 R2 R3 R4 熔点℃855  2-CF3-Ph          2-CH3-Ph    0 H  H   H   H   H856  3-CF3-Ph          2-CH3-Ph    0 H  H   H   H   H857  4-CF3-Ph          2-CH3-Ph    0 H  H   H   H   H858  4-(4-F-Ph)-Ph      4-F-Ph        0 H  H   H   H   H859  4-(2-Cl-Ph)-Ph     4-Cl-Ph       0 H  H   H   H   H860  3-(3-CF3-Ph)-Ph   2，4-F2-Ph  0 H  H   H   H   H861  3-(2，4-F2-Ph)-Ph 2，4-Cl2-Ph 0 H  H   H   H   H862  2，4-F2-Ph        4-CH3-Ph    0 H  H   H   H   H863  4-CH3-Ph          4-CH3-Ph    0 H  H   H   H   H   178-181.5864  2-CF3-Ph          4-CH3-Ph    0 H  H   H   H   H865  3-CF3-Ph          4-CH3-Ph    0 H  H   H   H   H866  4-CF3-Ph          4-CH3-Ph    0 H  H   H   H   H867  2-F-Ph             4-CH3O-Ph   0 H  H   H   H   H868  3-F-Ph             4-CH3O-Ph   0 H  H   H   H   H869  3-Cl-Ph            4-CH3O-Ph   0 H  H   H   H   H870  4-Br-Ph            4-CH3O-Ph   0 H  H   H   H   H871  2，4-F2-Ph        4-CH3O-Ph   0 H  H   H   H   H872  2，4-Cl2-Ph       4-CH3O-Ph   0 H  H   H   H   H873  2-CF3-Ph          4-CH3O-Ph   0 H  H   H   H   H874  3-CF3-Ph          4-CH3O-Ph   0 H  H   H   H   H875  4-CF3-Ph          4-CH3O-Ph   0 H  H   H   H   H876  Ph                 2-CH3O-Ph   0 H  H   H   H   H877  2-F-Ph             2-CH3O-Ph   0 H  H   H   H   H
      表I(续)实例号  A              B        n R   R1  R2  R3 R4 熔点℃878 3-F-Ph       2-CH3O-Ph    0 H   H    H    H   H879 4-F-Ph       2-CH3O-Ph    0 H   H    H    H   H    56-70
                                                   138-139.5
                                                  (·H2C2O4)880 2，4-F2-Ph  2-CH3O-Ph    0 H   H    H    H   H881 2-Cl-Ph      2-CH3O-Ph    0 H   H    H    H   H882 3-Cl-Ph      2-CH3O-Ph    0 H   H    H    H   H883 4-Cl-Ph      2-CH3O-Ph    0 H   H    H    H   H884 2，4-Cl2-Ph 2-CH3O-Ph    0 H   H    H    H   H885 4-Br-Ph      2-CH3O-Ph    0 H   H    H    H   H886 2-CF3-Ph    2-CH3O-Ph    0 H   H    H    H   H887 3-CF3-Ph    2-CH3O-Ph    0 H   H    H    H   H888 4-CF3-Ph    2-CH3O-Ph    0 H   H    H    H   H889 Ph           4-CF3O-Ph    0 H   H    H    H   H890 2-F-Ph       4-CF3O-Ph    0 H   H    H    H   H891 3-F-Ph       4-CF3O-Ph    0 H   H    H    H   H892 4-F-Ph       4-CF3O-Ph    0 H   H    H    H   H893 2，4-F2-Ph  4-CF3O-Ph    0 H   H    H    H   H894 2-Cl-Ph      4-CF3O-Ph    0 H   H    H    H   H895 3-Cl-Ph      4-CF3O-Ph    0 H   H    H    H   H896 4-Cl-Ph      4-CF3O-Ph    0 H   H    H    H   H897 2，4-Cl2-Ph 4-CF3O-Ph    0 H   H    H    H   H898 4-Br-Ph      4-CF3O-Ph    0 H   H    H    H   H899 2-CF3-Ph    4-CF3O-Ph    0 H   H    H    H   H
              表I(续)实例号  A              B        n R   R1 R2  R3 R4 熔点℃900 3-CF3-Ph    4-CF3O-Ph   0 H   H    H    H   H901 4-CF3-Ph    4-CF3O-Ph   0 H   H    H    H   H902 2-F-Ph       3，4-Cl2-Ph 0 H   H    H    H   H903 3-F-Ph       3，4-Cl2-Ph 0 H   H    H    H   H904 2，4-F2-Ph  3，4-Cl2-Ph 0 H   H    H    H   H905 3-Cl-Ph      3，4-Cl2-Ph 0 H   H    H    H   H    110-111906 2，4-Cl2-Ph 3，4-Cl2-Ph 0 H   H    H    H   H907 4-Br-Ph      3，4-Cl2-Ph 0 H   H    H    H   H908 2-CF3-Ph    3，4-Cl2-Ph 0 H   H    H    H   H909 3-CF3-Ph    3，4-Cl2-Ph 0 H   H    H    H   H910 4-CF3-Ph    3，4-Cl2-Ph 0 H   H    H    H   H911 Ph           2，5-F2-Ph  0 H   H    H    H   H912 2-F-Ph       2，5-F2-Ph  0 H   H    H    H   H913 3-F-Ph       2，5-F2-Ph  0 H   H    H    H   H914 4-F-Ph       2，5-F2-Ph  0 H   H    H    H   H915 2，4-F2-Ph  2，5-F2-Ph  0 H   H    H    H   H916 2-Cl-Ph      2，5-F2-Ph  0 H   H    H    H   H917 3-Cl-Ph      2，5-F2-Ph  0 H   H    H    H   H918 4-Cl-Ph      2，5-F2-Ph  0 H   H    H    H   H919 2，4-Cl2-Ph 2，5-F2-Ph  0 H   H    H    H   H920 4-Br-Ph      2，5-F2-Ph  0 H   H    H    H   H921 2-CF3-Ph    2，5-F2-Ph  0 H   H    H    H   H
               表I(续)实例号  A            B             n R  R1  R2  R3 R4熔点℃922 3-CF3-Ph    2，5-F2-Ph     0 H   H    H    H   H923 4-CF3-Ph    2，5-F2-Ph     0 H   H    H    H   H924 Ph           2，5-Cl2-Ph    0 H   H    H    H   H925 2-F-Ph       2，5-Cl2-Ph    0 H   H    H    H   H926 3-F-Ph       2，5-Cl2-Ph    0 H   H    H    H   H927 4-F-Ph       2，5-Cl2-Ph    0 H   H    H    H   H928 2，4-F2-Ph  2，5-Cl2-Ph    0 H   H    H    H   H929 2-Cl-Ph      2，5-Cl2-Ph    0 H   H    H    H   H930 3-Cl-Ph      2，5-Cl2-Ph    0 H   H    H    H   H931 4-Cl-Ph      2，5-Cl2-Ph    0 H   H    H    H   H932 2，4-Cl2-Ph 2，5-Cl2-Ph    0 H   H    H    H   H933 4-Br-Ph      2，5-Cl2-Ph    0 H   H    H    H   H934 2-CF3-Ph    2，5-Cl2-Ph    0 H   H    H    H   H935 3-CF3-Ph    2，5-Cl2-Ph    0 H   H    H    H   H936 4-CF3-Ph    2，5-Cl2-Ph    0 H   H    H    H   H937 Ph           2，4，6-F3-Ph  0 H   H    H    H   H938 2-F-Ph       2，4，6-F3-Ph  0 H   H    H    H   H939 3-F-Ph       2，4，6-F3-Ph  0 H   H    H    H   H940 4-F-Ph       2，4，6-F3-Ph  0 H   H    H    H   H941 2，4-F2-Ph  2，4，6-F3-Ph  0 H   H    H    H   H942 2-Cl-Ph      2，4，6-F3-Ph  0 H   H    H    H   H943 3-Cl-Ph      2，4，6-F3-Ph  0 H   H    H    H   H944 4-Cl-Ph      2，4，6-F3-Ph  0 H   H    H    H   H
             表I(续)实例号  A             B           n  R   R1 R2  R3 R4熔点℃945 2，4-Cl2-Ph 2，4，6-F3-Ph  0 H   H    H    H   H946 4-Br-Ph      2，4，6-F3-Ph  0 H   H    H    H   H947 2-CF3-Ph    2，4，6-F3-Ph  0 H   H    H    H   H948 3-CF3-Ph    2，4，6-F3-Ph  0 H   H    H    H   H949 4-CF3-Ph    2，4，6-F3-Ph  0 H   H    H    H   H950 Ph           2，4，5-F3-Ph  0 H   H    H    H   H951 2-F-Ph       2，4，5-F3-Ph  0 H   H    H    H   H952 3-F-Ph       2，4，5-F3-Ph  0 H   H    H    H   H953 4-F-Ph       2，4，5-F3-Ph  0 H   H    H    H   H954 2，4-F2-Ph  2，4，5-F3-Ph  0 H   H    H    H   H955 2-Cl-Ph      2，4，5-F3-Ph  0 H   H    H    H   H956 3-Cl-Ph      2，4，5-F3-Ph  0 H   H    H    H   H957 4-Cl-Ph      2，4，5-F3-Ph  0 H   H    H    H   H958 2，4-Cl2-Ph 2，4，5-F3-Ph  0 H   H    H    H   H959 4-Br-Ph      2，4，5-F3-Ph  0 H   H    H    H   H960 2-CF3-Ph    2，4，5-F3-Ph  0 H   H    H    H   H961 3-CF3-Ph    2，4，5-F3-Ph  0 H   H    H    H   H962 4-CF3-Ph    2，4，5-F3-Ph  0 H   H    H    H   H963 2-F-Ph       2-Cl-4-F-Ph      0 H   H    H    H   H964 3-F-Ph       2-Cl-4-F-Ph      0 H   H    H    H   H965 2，4-F2-Ph  2-Cl-4-F-Ph      0 H   H    H    H   H966 3-Cl-Ph      2-Cl-4-F-Ph      0 H   H    H    H   H967 2，4-Cl2-Ph 2-Cl-4-F-Ph      0 H   H    H    H   H968 4-Br-Ph      2-Cl-4-F-Ph      0 H   H    H    H   H
             表I(续)实例号  A                 B          n R   R1  R2  R3 R4熔点℃969 2-CF3-Ph       2-Cl-4-F-Ph    0 H   H    H    H   H970 3-CF3-Ph       2-Cl-4-F-Ph    0 H   H    H    H   H971 4-CF3-Ph       2-Cl-4-F-Ph    0 H   H    H    H   H972 Ph              4-F-1-萘基     0 H   H    H    H   H973 2-F-Ph          1-萘基         0 H   H    H    H   H974 3-F-Ph          1-″″         0 H   H    H    H   H975 4-F-Ph          1-″″         0 H   H    H    H   H976 2，4-F2-Ph     1-″″         0 H   H    H    H   H977 2-Cl-Ph         1-″″         0 H   H    H    H   H978 3-Cl-Ph         1-″″         0 H   H    H    H   H979 4-Cl-Ph         1-″″         0 H   H    H    H   H980 2，4-Cl2-Ph    1-″″         0 H   H    H    H   H981 4-Br-Ph         1-″″         0 H   H    H    H   H982 2-CF3-Ph       1-″″         0 H   H    H    H   H983 3-CF3-Ph       1-″″         0 H   H    H    H   H984 4-CF3-Ph       1-″″         0 H   H    H    H   H985 Ph              6-Cl-2-萘基    0 H   H    H    H   H986 2-F-Ph          2-萘基         0 H   H    H    H   H987 3-F-Ph          2-″″         0 H   H    H    H   H988 4-F-Ph          2-″″         0 H   H    H    H   H989 2，4-F2-Ph     2-″″         0 H   H    H    H   H990 2-Cl-Ph         2-″″         0 H   H    H    H   H991 3-Cl-Ph         2-″″         0 H   H    H    H   H992 4-Cl-Ph         2-″″         0 H   H    H    H   H993 2，4，-Cl2-Ph  2-″″         0 H   H    H    H   H994 4-Br-Ph         2-″″         0 H   H    H    H   H
             表I(续)实例号  A            B         n  R   R1  R2  R3 R4熔点℃995  2-CF3-Ph     2-萘基     0  H   H    H    H   H996  3-CF3-Ph     ″         0  H   H    H    H   H997  4-CF3-Ph     ″         0  H   H    H    H   H999  Ph            PhCH2-    0  H   H    H    H   H999  2-F-Ph        PhCH2-    0  H   H    H    H   H1000 3-F-Ph        PhCH2-    0  H   H    H    H   H1001 4-F-Ph        PnCH2-    0  H   H    H    H   H1002 2，4-F2-Ph   PhCH2-    0  H   H    H    H   H1003 2-Cl-Ph       PhCH2-    0  H   H    H    H   H1004 3-Cl-Ph       PhCH2-    0  H   H    H    H   H1005 4-Cl-Ph       PhCH2-    0  H   H    H    H   H1006 2，4-Cl2-Ph  PhCH2-    0  H   H    H    H   H1007 4-Br-Ph       PhCH2-    0  H   H    H    H   H1008 2-CF3-Ph     PhCH2-    0  H   H    H    H   H1009 3-CF3-Ph     PhCH2-    0  H   H    H    H   H1010 4-CF3-Ph     PhCH2-    0  H   H    H    H   H1011 Ph            PhCH(CH3) 0  H   H    H    H   H1012 2-F-Ph        PhCH(CH3) 0  H   H    H    H   H1013 3-F-Ph        PhCH(CH3) 0  H   H    H    H   H1014 4-F-Ph        PhCH(CH3) 0  H   H    H    H   H1015 2，4-F2-Ph   PhCH(CH3) 0  H   H    H    H   H1016 2-Cl-Ph       PhCH(CH3) 0  H   H    H    H   H
              表I(续)实例号  A             B                n   R  R1  R2 R3 R4熔点℃1017 3-Cl-Ph       PhCH(CH3)         0  H   H    H    H   H1018 4-Cl-Ph       PhCH(CH3)         0  H   H    H    H   H1019 2，4-Cl2-Ph  PhCH(CH3)         0  H   H    H    H   H1020 4-Br-Ph       PhCH(CH3)         0  H   H    H    H   H1021 2-CF3-Ph     PhCH(CH3)         0  H   H    H    H   H1022 3-CF3-Ph     PhCH(CH3)         0  H   H    H    H   H1023 4-CF3-Ph     PhCH(CH3)         0  H   H    H    H   H1024 Ph            PhC(CH3)2-       0  H   H    H    H   H1025 2-F-Ph        PhC(CH3)2-       0  H   H    H    H   H1026 3-F-Ph        PhC(CH3)2-       0  H   H    H    H   H1027 4-F-Ph        PhC(CH3)2-       0  H   H    H    H   H1028 2，4-F2-Ph   PhC(CH3)2-       0  H   H    H    H   H1029 2-Cl-Ph       PhC(CH3)2-       0  H   H    H    H   H1030 3-Cl-PH       PhC(CH3)2-       0  H   H    H    H   H1031 4-Cl-Ph       PhC(CH3)2-       0  H   H    H    H   H1032 2，4-Cl2-Ph  PhC(CH3)2-       0  H   H    H    H   H1033 4-Br-Ph       PhC(CH3)2-       0  H   H    H    H   H1034 2-CF3-Ph     PhC(CH3)2-       0  H   H    H    H   H1035 3-CF3-Ph     PhC(CH3)2-       0  H   H    H    H   H1036 4-CF3-Ph     PhC(CH3)2-       0  H   H    H    H   H1037 Ph            4-Cl-PhC(CH3)2-  0  H   H    H    H   H1038 2-F-Ph        4-Cl-PhC(CH3)2-  0  H   H    H    H   H
        表I(续)实例号  A              B                n  R  R1  R2 R3 R4熔点℃1039 3-F-Ph        4-Cl-PhC(CH3)2-  0  H   H    H   H   H1040 4-F-Ph        4-Cl-PhC(CH3)2-  0  H   H    H   H   H1041 2，4-F2-Ph   4-Cl-PhC(CH3)2-  0  H   H    H   H   H1042 2-Cl-Ph       4-Cl-PhC(CH3)2-  0  H   H    H   H   H1043 3-C1-Ph       4-Cl-PhC(CH3)2-  0  H   H    H   H   H1044 4-Cl-Ph       4-Cl-PhC(CH3)2-  0  H   H    H   H   H1045 2，4-Cl2-Ph  4-Cl-PhC(CH3)2-  0  H   H    H   H   H1046 4-Br-Ph       4-Cl-PhC(CH3)2-  0  H   H    H   H   H1047 2-CF3-Ph     4-Cl-PhC(CH3)2-  0  H   H    H   H   H1048 3-CF3-Ph     4-Cl-PhC(CH3)2-  0  H   H    H   H   H1049 4-CF3-Ph     4-Cl-PhC(CH3)2-  0  H   H    H   H   H1050 Ph             2-噻吩基           0  H   H    H   H   H1051 2-F-Ph         2-″″″           0  H   H    H   H   H1052 3-F-Ph         2-″″″           0  H   H    H   H   H1053 4-F-Ph         2-″″″           0  H   H    H   H   H1054 2，4-F2-Ph    2-″″″           0  H   H    H   H   H1055 2-Cl-Ph        2-″″″           0  H   H    H   H   H1056 3-Cl-Ph        2-″″″           0  H   H    H   H   H1057 4-Cl-Ph        2-″″″           0  H   H    H   H   H1058 2，4-Cl2-Ph   2-″″″           0  H   H    H   H   H1059 4-Br-Ph        2-″″″           0  H   H    H   H   H1060 2-CF3-Ph      2-″″″           0  H   H    H   H   H1061 3-CF3-Ph      2-″″″           0  H   H    H   H   H1062 4-CF3-Ph      2-″″″           0  H   H    H   H   H
               表I(续)实例号   A          B               n R   R1 R2 R3 R4熔点℃1063 Ph           3-噻吩基         0 H   H    H   H   H1064 2-F-Ph       3-″″″         0 H   H    H   H   H1065 3-F-Ph       3-″″″         0 H   H    H   H   H1066 4-F-Ph       3-″″″         0 H   H    H   H   H1067 2，4-F2-Ph  3-″″″         0 H   H    H   H   H1068 2-Cl-Ph      3-″″″         0 H   H    H   H   H1069 3-Cl-Ph      3-″″″         0 H   H    H   H   H1070 4-Cl-Ph      3-″″″         0 H   H    H   H   H1071 2，4-Cl2-Ph 3-″″″         0 H   H    H   H   H1072 4-Br-Ph      3-″″″         0 H   H    H   H   H1073 2-CF3-Ph    3-″″″         0 H   H    H   H   H1074 3-CF3-Ph    3-″″″         0 H   H    H   H   H1075 4-CF3-Ph    3-″″″         0 H   H    H   H   H1076 2-F-Ph       2-Cl-3-噻吩基    0 H   H    H   H   H1077 3-F-Ph       2-Cl-3-″″″    0 H   H    H   H   H1078 2，4-F2-Ph  2-Cl-3-″″″    0 H   H    H   H   H1079 3-Cl-Ph      2-Cl-3-″″″    0 H   H    H   H   H1080 2，4-Cl2-Ph 2-Cl-3-″″″    0 H   H    H   H   H1081 4-Br-Ph      2-Cl-3-″″″    0 H   H    H   H   H1082 2-CF3-Ph    2-Cl-3-″″″    0 H   H    H   H   H1083 3-CF3-Ph    2-Cl-3-″″″    0 H   H    H   H   H1084 4-CF3-Ph    2-Cl-3-″″″    0 H   H    H   H   H1085 2-F-Ph       5-Cl-2-″″″    0 H   H    H   H   H1086 3-F-Ph       5-Cl-2-″″″    0 H   H    H   H   H1087 2，4-F2-Ph  5-Cl-2-″″″    0 H   H    H   H   H
           表I(续)实例号  A            B                n R   R1  R2 R3 R4 熔点℃1088 3-Cl-Ph       5-Cl-2-噻吩基      0 H   H    H    H   H1089 2，4-Cl2-Ph  5-Cl-2-″″″      0 H   H    H    H   H1090 4-Br-Ph       5-Cl-2-″″″      0 H   H    H    H   H1091 2-CF3-Ph     5-Cl-2-″″″      0 H   H    H    H   H1092 3-CF3-Ph     5-Cl-2-″″″      0 H   H    H    H   H1093 4-CF3-Ph     5-Cl-2-″″″      0 H   H    H    H   H1094 Ph            2，5-Cl2-3-噻吩基 0 H   H    H    H   H1095 2-F-Ph        2，5-Cl2-3-″″″ 0 H   H    H    H   H1096 3-F-Ph        2，5-Cl2-3-″″″ 0 H   H    H    H   H1097 4-F-Ph        2，5-Cl2-3-″″″ 0 H   H    H    H   H  60-621098 2，4-F2-Ph   2，5-Cl2-3-″″″ 0 H   H    H    H   H1099 2-Cl-Ph       2，5-Cl2-3-″″″ 0 H   H    H    H   H1100 3-Cl-Ph       2，5-Cl2-3-″″″ 0 H   H    H    H   H1101 4-Cl-Ph       2，5-Cl2-3-″″″ 0 H   H    H    H   H1102 2，4-Cl2-Ph  2，5-Cl2-3-″″″ 0 H   H    H    H   H1103 4-Br-Ph       2，5-Cl2-3-″″″ 0 H   H    H    H   H1104 2-CF3-Ph     2，5-Cl2-3-″″″ 0 H   H    H    H   H1105 3-CF3-Ph     2，5-Cl2-3-″″″ 0 H   H    H    H   H1106 4-CF3-Ph     2，5-Cl2-3-″″″ 0 H   H    H    H   H1107 Ph            5-溴-2-″″″       0 H   H    H    H   H1108 2-F-Ph        5-″-2-″″″       0 H   H    H    H   H1109 3-F-Ph        5-″-2-″″″       0 H   H    H    H   H1110 4-F-Ph        5-″-2-″″″       0 H   H    H    H   H1111 2，4-F2-Ph   5-″-2-″″″       0 H   H    H    H   H
               表I(续)实例号  A                B         n R   R1  R2 R3  R4熔点℃1112 2-Cl-Ph       5-溴-2-噻吩基  0 H   H    H    H   H1113 3-Cl-Ph       5-″ ″  ″    0 H   H    H    H   H1114 4-Cl-Ph       5-″ ″  ″    0 H   H    H    H   H1115 2，4-Cl2-Ph  5-″ ″  ″    0 H   H    H    H   H1116 4-Br-Ph       5-″ ″  ″    0 H   H    H    H   H1117 2-CF3-Ph     5-″ ″  ″    0 H   H    H    H   H1118 3-CF3-Ph     5-″ ″  ″    0 H   H    H    H   H1119 4-CF3-Ph     5-″ ″  ″    0 H   H    H    H   H1120 Ph            2-吡啶基       0 H   H    H    H   H1121 2-F-Ph        2-″″″       0 H   H    H    H   H1122 3-F-Ph        2-″″″       0 H   H    H    H   H1123 2，4-F2-Ph   2-″″″       0 H   H    H    H   H1124 2-Cl-Ph       2-″″″       0 H   H    H    H   H1125 3-Cl-Ph       2-″″″       0 H   H    H    H   H1126 4-Cl-Ph       2-″″″       0 H   H    H    H   H1127 2，4-Cl2-Ph  2-″″″       0 H   H    H    H   H1128 4-Br-Ph       2-″″″       0 H   H    H    H   H1129 2-CF3-Ph     2-″″″       0 H   H    H    H   H1130 3-CF3-Ph     2-″″″       0 H   H    H    H   H1131 4-CF3-Ph     2-″″″       0 H   H    H    H   H1132 Ph            3-″″″       0 H   H    H    H   H1133 2-F-Ph        3-″″″       0 H   H    H    H   H1134 3-F-Ph        3-″″″       0 H   H    H    H   H1135 4-F-Ph        3-″″″       0 H   H    H    H   H1136 2，4-F2-Ph   3-″″″       0 H   H    H    H   H1137 2-Cl-Ph       3-″″″       0 H   H    H    H   H
            表I(续)实例号  A              B           n R   R1  R2 R3  R4熔点℃1138 3-Cl-Ph       3-吡啶基       0 H   H    H    H    H1139 4-Cl-Ph       3-″″″       0 H   H    H    H    H1140 2，4-Cl2-Ph  3-″″″       0 H   H    H    H    H1141 4-Br-Ph       3-″″″       0 H   H    H    H    H1142 2-CF3-Ph     3-″″″       0 H   H    H    H    H1143 3-CF3-Ph     3-″″″       0 H   H    H    H    H1144 4-CF3-Ph     3-″″″       0 H   H    H    H    H1145 Ph            4-″″″       0 H   H    H    H    H1146 2-F-Ph        4-″″″       0 H   H    H    H    H1147 3-F-Ph        4-″″″       0 H   H    H    H    H1148 2，4-F2-Ph   4-″″″       0 H   H    H    H    H1149 2-Cl-Ph       4-″″″       0 H   H    H    H    H1150 3-Cl-Ph       4-″″″       0 H   H    H    H    H1151 4-Cl-Ph       4-″″″       0 H   H    H    H    H1152 2，4-Cl2-Ph  4-″″″       0 H   H    H    H    H1153 4-Br-Ph       4-″″″       0 H   H    H    H    H1154 2-CF3-Ph     4-″″″       0 H   H    H    H    H1155 3-CF3-Ph     4-″″″       0 H   H    H    H    H1156 4-CF3-Ph     4-             0 H   H    H    H    H1157 Ph            2-Cl-3-吡啶基  0 H   H    H    H    H1158 2-F-Ph        2-Cl-3-″″″  0 H   H    H    H    H1159 3-F-Ph        2-Cl-3-″″″  0 H   H    H    H    H1160 4-F-Ph        2-Cl-3-″″″  0 H   H    H    H    H1161 2，4-F2-Ph   2-Cl-3-″″″  0 H   H    H    H    H1162 2-Cl-Ph       2-Cl-3-″″″  0 H   H    H    H    H1163 3-Cl-Ph       2-Cl-3-″″″  0 H   H    H    H    H1164 4-Cl-Ph       2-Cl-3-″″″  0 H   H    H    H    H1165 2，4-Cl2-Ph  2-Cl-3-″″″  0 H   H    H    H    H
               表I(续)实例号  A              B           n R   R1 R2 R3 R4 熔点℃1166 4-Br-Ph       2-Cl-3-吡啶基  0 H   H   H    H   H1167 2-CF3-Ph     2-Cl-3-″″″  0 H   H   H    H   H1168 3-CF3-Ph     2-Cl-3-″″″  0 H   H   H    H   H1169 4-CF3-Ph     2-Cl-3-″″″  0 H   H   H    H   H1170 Ph            3-Cl-2-″″″  0 H   H   H    H   H1171 2-F-Ph        3-Cl-2-″″″  0 H   H   H    H   H1172 3-F-Ph        3-Cl-2-″″″  0 H   H   H    H   H1173 4-F-Ph        3-Cl-2-″″″  0 H   H   H    H   H1174 2，4-F2-Ph   3-Cl-2-″″″  0 H   H   H    H   H1175 2-Cl-Ph       3-Cl-2-″″″  0 H   H   H    H   H1176 3-Cl-Ph       3-Cl-2-″″″  0 H   H   H    H   H1177 4-Cl-Ph       3-Cl-2-″″″  0 H   H   H    H   H1178 2，4-Cl2-Ph  3-Cl-2-″″″  0 H   H   H    H   H1179 4-Br-Ph       3-Cl-2-″″″  0 H   H   H    H   H1180 2-CF3-Ph     3-Cl-2-″″″  0 H   H   H    H   H1181 3-CF3-Ph     3-Cl-2-″″″  0 H   H   H    H   H1182 4-CF3-Ph     3-Cl-2-″″″  0 H   H   H    H   H1183 2-F-Ph        5-Cl-2-″″″  0 H   H   H    H   H1184 3-F-Ph        5-Cl-2-″″″  0 H   H   H    H   H1185 2，4-F-Ph     5-Cl-2-″″″  0 H   H   H    H   H1186 3-Cl-Ph       5-Cl-2-″″″  0 H   H   H    H   H1187 2，4-Cl2-Ph  5-Cl-2-″″″  0 H   H   H    H   H1188 4-Br-Ph       5-Cl-2-″″″  0 H   H   H    H   H1189 2-CF3-Ph     5-Cl-2-″″″  0 H   H   H    H   H1190 3-CF3-Ph     5-Cl-2-″″″  0 H   H   H    H   H1191 4-CF3-Ph     5-Cl-2-″″″  0 H   H   H    H   H1192 Ph            6-Cl-3-″″″  0 H   H   H    H   H
                       表I(续)实例号  A                     B             n R   R1 R2  R3 R4  熔点℃1193 2-F-Ph             6-Cl-3-吡啶基      0 H   H    H    H   H1194 3-F-Ph             6-Cl-3-″″″      0 H   H    H    H   H1195 4-F-Ph             6-Cl-3-″″″      0 H   H    H    H   H1196 2，4-F2-Ph        6-Cl-3-″″″      0 H   H    H    H   H1197 2-Cl-Ph            6-Cl-3-″″″      0 H   H    H    H   H1198 3-Cl-Ph            6-Cl-3-″″″      0 H   H    H    H   H1199 4-Cl-Ph            6-Cl-3-″″″      0 H   H    H    H   H1200 2，4-Cl2-Ph       6-Cl-3-″″″      0 H   H    H    H   H1201 4-Br-Ph            6-Cl-3-″″″      0 H   H    H    H   H1202 2-CF3-Ph          6-Cl-3-″″″      0 H   H    H    H   H1203 3-CF3-Ph          6-Cl-3-″″″      0 H   H    H    H   H1204 4-CF3-Ph          6-Cl-3-″″″      0 H   H    H    H   H1205 2-噻吩基           2-噻吩基           0 H   H    H    H   H1206 3-″″″           2-″″″           0 H   H    H    H   H1207 2-Cl-3-噻吩基      2-″″″           0 H   H    H    H   H1208 5-Cl-2-″″″      2-″″″           0 H   H    H    H   H1209 2，5-Cl2-3-″″″ 2-″″″           0 H   H    H    H   H1210 2-噻吩基           3-″″″           0 H   H    H    H   H1211 3-″″″           3-″″″           0 H   H    H    H   H1212 2-Cl-3-噻吩基      3-″″″           0 H   H    H    H   H1213 5-Cl-2-″″″      3-″″″           0 H   H    H    H   H1214 2，5-Cl2-3-″″″ 3-″″″           0 H   H    H    H   H1215 2-噻吩基           2-Cl-3-噻吩基      0 H   H    H    H   H1216 3-″″″           2-Cl-3-″″″      0 H   H    H    H   H1217 2-Cl-3-噻吩基      2-Cl-3-″″″      0 H   H    H    H   H1218 5-Cl-2-″″″      2-Cl-3-″″″      0 H   H    H    H   H1219 2，5-Cl2-3-″″″ 2-Cl-3-″″″      0 H   H    H    H   H1220 2-噻吩基           5-Cl-3-″″″      0 H   H    H    H   H
              表I(续)实例号  A                    B               n   R   R1 R2 R3       R41221 3-噻吩基           5-Cl-3-噻吩基       0   H   H   H    H         H1222 2-Cl-3-″″″      5-Cl-3-″″″       0   H   H   H    H         H1223 5-Cl-2-″″″      5-Cl-3-″″″       0   H   H   H    H         H1224 2，5-Cl2-3-″″″ 5-Cl-3-″″″       0   H   H   H    H         H1225 2-噻吩基           2，5-Cl2-3-噻吩基  0   H   H   H    H         H1226 3-″″″           2，5-Cl2-3-″″″  0   H   H   H    H         H1227 2-Cl-3-thienyl     2，5-Cl2-3-″″″  0   H   H   H    H         H1228 5-Cl-2-″″″      2，5-Cl2-3-″″″  0   H   H   H    H         H1229 2，5-Cl2-3-″″″ 12，5-Cl2-3-″″″ 0   H   H   H    H         H1230 噻吩基             5-F-2-噻吩基         0   H   H   H    H         H1231 3-吡啶基           5-Cl-2-吡啶基        0   H   H   H    H         H1232 5-Cl-2-吡啶基      5-Cl-2-″″″        0   H   H   H    H         H1233 4-吡啶基           5-Cl-2-″″″        0   H   H   H    H         H1234 2-Cl-3-″″″      5-Cl-2-″″″        0   H   H   H    H         H1235 2-吡啶基           5-Cl-2-″″″        0   H   H   H    H         H1236 4-F-Ph             4-F-Ph               0   H   H   H    C2H5   H1237 4-F-Ph             4-F-Ph               0   H   H   H    n-C3H7 H1238 4-F-Ph             4-F-Ph               0   H   H   H    n-C4H9 H1239 4-F-Ph             4-F-Ph               0   H   H   H    i-C3H7 H1240 4-F-Ph             4-F-Ph               0   H   H   H    s-C4H9 H1241 2-Cl-Ph            4-Cl-Ph              0   H   H   H    C2H5   H1242 2-Cl-Ph            4-Cl-Ph              0   H   H   H    n-C3H7 H1243 2-Cl-Ph            4-Cl-Ph              0   H   H   H    n-C4H9 H1244 2-Cl-Ph            4-Cl-Ph              0   H   H   H    i-C3H7 H1245 2-Cl-Ph            4-Cl-Ph              0   H   H   H    s-C4H9 H1246 4-Cl-Ph            2，4-Cl2-Ph         0   H   H   H    C2H5   H
             表I(续)实例号  A          B         n  R   R1 R2 R3       R4     熔点℃1247 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   n-C3H7  H1248 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   n-C4H9  H1249 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   i-C3H7  H1250 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   s-C4H9  H1251 Ph       4-F-Ph        0  H   H   H   C2H5    H1252 Ph       4-F-Ph        0  H   H   H   n-C3H7  H1253 Ph       4-F-Ph        0  H   H   H   n-C4H9  H1254 Ph       4-F-Ph        0  H   H   H   i-C3H7  H1255 Ph       4-F-Ph        0  H   H   H   s-C4H9  H1256 4-F-Ph   4-F-Ph        0  H   H   H   CH3      H1257 4-F-Ph   4-F-Ph        0  H   H   H   CH3      CH31258 4-F-Ph   4-F-Ph        0  H   H   H   F         H        166-1671259 4-F-Ph   4-F-Ph        0  H   H   H   F         CH31260 4-F-Ph   4-F-Ph        0  H   H   H   F         F        145-1471261 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   CH3     H1262 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   CH3     CH31263 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   F        H1264 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   F        CH31265 4-Cl-Ph  2，4-Cl2-Ph  0  H   H   H   F        F1266 2-Cl-Ph  4-Cl-Ph       0  H   H   H   CH3     H1267 2-Cl-Ph  4-Cl-Ph       0  H   H   H   CH3     CH31268 2-Cl-Ph  4-Cl-Ph       0  H   H   H   F        H1269 2-Cl-Ph  4-Cl-Ph       0  H   H   H   F        CH31270 2-Cl-Ph  4-Cl-Ph       0  H   H   H   F        F
                 表I(续)实例号A       B       n  R  R1 R2  R3 R4  熔点℃1271 Ph    4-F-Ph    0  H  H   H    CH3 H1272 Ph    4-F-Ph    0  H  H   H    CH3 CH31273 Ph    4-F-Ph    0  H  H   H    F    H1274 Ph    4-F-Ph    0  H  H   H    F    CH31275 Ph    4-F-Ph    0  H  H   H    F    Fa  NMR：(CDCl3)δ4.70(q，J＝4Hz，2H)；4.90
  (s，1H)；5.40(s，1H)；5.55(s，1H)；6.8-7.0
  (m，4H)；7.2-7.4(m，4H)，7.8(bs，2H).b  NMR：(CDCl3)δ4.8(q，2H)，5.2(s，1H)，
  5.3(s，1H)，5.6(s，1H)，6.9-7.6(m，8H)，7.8
  (s，1H)，8.1(s，1H).c  NMR：(CDCl3)δ4.70(q，J＝13Hz，2H)；4.85
  (s，1H)；5.35(s，1H)；5.55(s，1H)；6.85-7.4
  (m，8H)；7.7(s，H)；7.9(s，1H).d  NMR：(CDCl3)δ4.60(q，J＝12Hz，2H)；5.0
  (s，1H)；5.40(s，1H)；5.55(s，1H)；6.8(1/2
  of ABq，J＝10Hz，2H)；7.00(m，2H)；7.3(1/2 of
  ABq，J＝10Hz，2H)；7.45(m，2H)；7.80(s，1H)；
  7.85(s，1H).e  NMR：(CDCl3)δ4.6，4.8(ABq，J＝14Hz，2H)；
  4.9(br s，3H)；5.3(s，1H)；5.6(s，1H)；6.8
  (d，1H)；7.0(m，3H)；7.4(m，3H)；7.8(s，1H)；
  7.9(s，1H).  f NMR：(CDCl3)δ1.3(s，9H)，4.7(q，2H)，
4.6(s，1H)，5.0(s，1H)，5.4(s，1H)，6.8-7.4
(9H)，7.8(s，1H).g NMR：(CDCl3)δ4.7，4.8(ABq，J＝12Hz，2H)；
6.7-7.5(m，14H)；7.9(s，1H)；8.0(s，1H).h NMR：(CDCl3)δ3.45(s，3H)；4.75(ABq，
J＝18Hz，14Hz，2H)；4.6(m，2H)；6.8-7.0(m，4H)；
7.05-7.25(m，4H)；8.0(s，1H)；8.25(s，1H).i NMR：(CDCl3)δ4.0(dd，14，4Hz，1H)；4.3
(dd，14，4Hz，1H)；4.6(d，13Hz，1H)；4.9(d，
13Hz，1H)；5.1(d，1H)；5.3(d，1H)；5.55(s，
1H)；5.60(s，1H)；5.85(m，1H)；6.8-7.0(m，
4H)；7.05-7.2(m，4H)；8.05(s，1H)；8.25(s，
1H).j NMR：(CDCl3)δ1.90(s，3H)；4.80(1/2 of
ABq，J＝14Hz，1H)；5.65(1/2 of ABq，J＝14Hz，1H)；
5.55(s，1H)；5.60(s，1H)；6.75-7.0(m，4H)；
7.0-7.2(t，2H)；7.25-7.4(m，2H)；7.35(s，1H)；
7.85(s，1H).k NMR：(CDCl3)δ4.03，4.11(ABq，J＝11Hz，
2H)；4.25(s，1H，0H)；4.39(s，1H，0H)，4.54，
4.81(ABq，J＝14Hz，2H)；5.31，5.33(2 sharp s，
1H each)；7.25-7.40(m，4H)；7.71(s，1H)；8.03
(s，1H).l NMR：(CDCl3)δ2.03(s，1H，0H)；4.0-4.2(m，2H)；4.57，4.85(ABq，J＝15Hz，2H)；5.3-5.35(m，2H)；5.7-5.9(broad s，1H，0H)；7.3-7.6(m，4H)；7.75(s，1H)；8.11(s，1H).m NMR：(CDCl3)δ2.10(s，6H)；2.52，3.03(ABq，J＝12Hz，2H)；4.41，4.78(ABq，J＝15Hz，2H)；5.19(s，1H)；5.50(s，1H)；6.9-7.2(m，2H)；7.4-7.6(m，2H)；7.80(s，1H)；8.36(s，1H).n NMR：(CDCl3)δ2.11(s，6H)；2.61，3.11(ABq，J＝12Hz，2H)；4.50，4.90(ABq，J＝13Hz，2H)；5.13(s，1H)；5.50(s，1H)；7.50(s，4H)；7.86(s，1H)；8.14(s，1H).o NMR：(CDCl3)δ2.13(s，3H)；2.19(s，3H)；2.5-3.1(m，2H)；4.44，4.85(ABq，J＝14Hz，2H)；5.0-5.5(m，2H)；7.3-7.8(m，9H)；7.97(s，1H)；8.32(s，1H，0H)；8.50(s，1H).p NMR：(CDCl3)δ4.6(d，1/2 of ABq，1H)；4.9(d，1/2 of ABq，1H)；5.0(s，1H)；5.3(two s，2H)；6.9-7.6(m，9H)；7.8(two s，2H).q NMR：(CDCl3)δ1.0(t，3H)；1.2(s，1H)；1.6(m，2H)；4.2(ABq，2H)；5.1(s，1H)；5.4(s，1H)；6.9-7.1(m，4H)；7.9(s，1H)；8.0(s，1H).
实例1276和1276a：实例49的(S)一对映体制备：
把实例49化合物(1.5克)和1.5克1-α-溴樟脑-π-磺酸溶于75毫升的乙腈并回流2小时。冷却溶液至室温并静置14小时。用另外部分的乙腈对过泸的得固体进行重结晶，得1.28克白色固体，熔点216-217℃；〔α〕D 25＝-104〔C＝1；DMSO)。
蒸发乙腈得到加成化合物具有(+)旋光性(实例1276a)。可用乙醚/丙酮混合物对该化合物进行重结晶得一固体，接着用NaHCO3水溶液处理，经NMR鉴定为实例49的化合物。
把上述固体悬浮于50毫升的NaHCO3饱和溶液和剧烈搅拌至产生的产生气体消失(1-2小时)。混合物用50毫升CHCl3萃取2次。合并有机层用盐水洗涤，Na2SO4干燥并真空蒸发溶剂。这样得到750毫克白色固体(实例1276)，6HNMR鉴定为实例49化合物，熔点＝82-83℃；〔α〕D 25＝-62·(C＝1；CHCl3)。
表2列出上面描述被溶介的这些化物以及其它化合物。实例号            A           B        n   R   R1  R2 R3  R4 熔点℃    [α]D 251276           
Figure C9210593000782
   0   H   H    H    H    H   82-83       -62°1276a(1)           0   H   H    H    H    H   83-84       +60°1277(2)     
Figure C9210593000784
     0   H   H    H    H    H   60-61       -67°
                                                            (HCl salt
                                                             181-184)1277a(1)，(2) 
Figure C9210593000785
     0   H   H    H    H    H   60-62       +66°*表示手性中心。(1)＝取代d-α-溴代樟脑-π-磺酸(2)＝使用一个其中3部分乙醚-1部分丙酮的混合物为溶剂。
实例12782-(4-氟苯基)-3-苯基-1-(5-巯基-1H-1，2，4-三唑-1-基)-3-丁烯-1-醇
在-70℃于5分钟向1.24克(0.004摩尔)2-(4-氟苯基)-3-苯基-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇的15毫升THF溶液加入5.2毫升(0.008摩尔)的1.55克分子浓度正丁基锂的己烷溶液。30分钟后，加入0.13克(0.004摩尔)硫，加热反应混合液至室温1小时，然后用8毫升1当量HCl骤冷。混合物注入饱和NH4Cl后，用醚萃取2次，合并有机相用盐水洗涤，Na2SO4干燥并蒸发。粗产品用闪色谱层析纯化，用2∶13∶85甲醇/醚/二氯甲烷洗脱得0.85克标题化合物，熔点54-58℃：NMR(CDCl)δ4.7(A βq，2h)，5.0(S，1H，OH)，5.3(S，1H，乙烯基)，5.5(S，1H，乙烯基)，7.0(m，4H)，7.2(m，3H)，7.5(m，2H)，7.7(s，1H，三唑部分)，12.5(brs.1H，SH)；IR(二氯甲烷)3500-3000(宽)，1590，1500，1465，1230，1162，1109，825厘米-1；MS：最高m/e 341。
表3中所列化合物已用上述方法制备或可以制备得到。
表3
Figure C9210593000801
实例号 A         B           R R1  R2 R4 Q   熔点℃1278  Ph      4-F-Ph        H H    H    H   SH  54-581279  Ph      Ph            H H    H    H   SH1280  Ph      2-F-Ph        H H    H    H   SH1281  Ph      2-Cl-Ph       H H    H    H   SH1282  Ph      4-Cl-Ph       H H    H    H   SH1283  Ph      2，4-F2-Ph   H H    H    H   SH1284  Ph      2，4-Cl2-Ph  H H    H    H   SH1285  2-F-Ph  Ph            H H    H    H   SH1286  2-F-Ph  2-F-Ph        H H    H    H   SH1287  2-F-Ph  4-F-Ph        H H    H    H   SH1288  2-F-Ph  2-Cl-Ph       H H    H    H   SH1289  2-F-Ph  4-Cl-Ph       H H    H    H   SH1290  2-F-Ph  2，4-F2-Ph   H H    H    H   SH1291  2-F-Ph  2，4-Cl2-Ph  H H    H    H   SH1292  3-F-Ph  Ph            H H    H    H   SH1293  3-F-Ph  2-F-Ph        H H    H    H   SH1294  3-F-Ph  4-F-Ph        H H    H    H   SH1295  3-F-Ph  2-Cl-Ph       H H    H    H   SH1296  3-F-Ph  4-Cl-Ph       H H    H    H   SH1297  3-F-Ph  2，4-F2-Ph   H H    H    H   SH1298  3-F-Ph  2，4-Cl2-Ph  H H    H    H   SH1299  4-F-Ph  Ph            H H    H    H   SH1300  4-F-Ph  2-F-Ph        H H    H    H   SH  144.5-1481301  4-F-Ph  4-F-Ph        H H    H    H   SH1302  4-F-Ph  2-Cl-Ph       H H    H    H   SH
           表3(续)实例号   A           B          R  R1 R2 R4 Q  熔点℃1303  4-F-Ph     4-Cl-Ph       H  H   H    H   SH1304  4-F-Ph     2，4-F2-Ph   H  H   H    H   SH (foam)a1305  4-F-Ph     2，4-Cl2-Ph  H  H   H    H   SH1308  2-Cl-Ph    4-F-Ph        H  H   H    H   SH1311  2-Cl-Ph    2，4-F2-Ph   H  H   H    H   SH1312  2-Cl-Ph    2，4-Cl2-Ph  H  H   H    H   SH1318  3-Cl-Ph    2，4-F2-Ph   H  H   H    H   SH1319  3-Cl-Ph    2，4-Cl2-Ph  H  H   H    H   SH1323  4-Cl-Ph    2-Cl-Ph       H  H   H    H   SH1324  4-Cl-Ph    4-Cl-Ph       H  H   H    H   SH1325  4-Cl-Ph    2，4-F2-Ph   H  H   H    H   SH1326  4-Cl-Ph    2，4-Cl2-Ph  H  H   H    H   SH1327  2-CF3-Ph  Ph            H  H   H    H   SH1328  2-CF3-Ph  2-F-Ph        H  H   H    H   SH1329  2-CF3-Ph  4-F-Ph        H  H   H    H   SH
        表3(续)实例号    A           B         R  R1 R2 R4 Q  熔点℃1330 2-CF3-Ph    2-Cl-Ph      H  H   H    H  SH1331 2-CF3-Ph    4-Cl-Ph      H  H   H    H  SH1332 2-CF3-Ph    2，4-F2-Ph  H  H   H    H  SH1333 2-CF3-Ph    2，4-Cl2-Ph H  H   H    H  SH1334 4-CF3-Ph    Ph           H  H   H    H  SH1335 4-CF3-Ph    2-F-Ph       H  H   H    H  SH1336 4-CF3-Ph    4-F-Ph       H  H   H    H  SH1337 4-CF3-Ph    2-Cl-Ph      H  H   H    H  SH1338 4-CF3-Ph    4-Cl-Ph      H  H   H    H  SH1339 4-CF3-Ph    2，4-F2-Ph  H  H   H    H  SH1340 4-CF3-Ph    2，4-Cl2-Ph H  H   H    H  SH1341 2，4-F2-Ph  Ph           H  H   H    H  SH1342 2，4-F2-Ph  2-F-Ph       H  H   H    H  SH1343 2，4-F2-Ph  4-F-Ph       H  H   H    H  SH1344 2，4-F2-Ph  2-Cl-Ph      H  H   H    H  SH1345 2，4-F2-Ph  4-Cl-Ph      H  H   H    H  SH1346 2，4-F2-Ph  2，4-F2-Ph  H  H   H    H  SH1347 2，4-F2-Ph  2，4-Cl2-Ph H  H   H    H  SH1348 2，4-Cl2-Ph Ph           H  H   H    H  SH1349 2，4-Cl2-Ph 2-F-Ph       H  H   H    H  SH1350 2，4-Cl2-Ph 4-F-Ph       H  H   H    H  SH1351 2，4-Cl2-Ph 2-Cl-Ph      H  H   H    H  SH1352 2，4-Cl2-Ph 4-Cl-Ph      H  H   H    H  SH
              表3(续)实例号    A            B           R  R1 R2  R4 Q   熔点℃1353  2，4-Cl2-Ph 2，4-F2-Ph   H   H   H    H   SH1354  2，4-Cl2-Ph 2，4-Cl2-Ph  H   H   H    H   SH1355  Ph           Ph             H   H   H    H   I1356  Ph           2-F-Ph         H   H   H    H   I1357  Ph           4-F-Ph         H   H   H    H   I1358  Ph           2-Cl-Ph        H   H   H    H   I1359  Ph           4-Cl-Ph        H   H   H    H   I1360  Ph           2，4-F2-Ph    H   H   H    H   I1361  Ph           2，4-Cl2-Ph   H   H   H    H   I1362  2-F-Ph       Ph             H   H   H    H   I1363  2-F-Ph       2-F-Ph         H   H   H    H   I1364  2-F-Ph       4-F-Ph         H   H   H    H   I1365  2-F-Ph       2-Cl-Ph        H   H   H    H   I1366  2-F-Ph       4-Cl-Ph        H   H   H    H   I1367  2-F-Ph       2，4-F2-Ph    H   H   H    H   I1368  2-F-Ph       2，4-Cl2-Ph   H   H   H    H   I1369  3-F-Ph       Ph             H   H   H    H   I1370  3-F-Ph       2-F-Ph         H   H   H    H   I1371  3-F-Ph       4-F-Ph         H   H   H    H   I1372  3-F-Ph       2-Cl-Ph        H   H   H    H   I1373  3-F-Ph       4-Cl-Ph        H   H   H    H   I1374  3-F-Ph       2，4-F2-Ph    H   H   H    H   I1375  3-F-Ph       2，4-Cl2-Ph   H   H   H    H   I1376  4-F-Ph       Ph             H   H   H    H   I1377  4-F-Ph       2-F-Ph         H   H   H    H   I   96-97.51378  4-F-Ph       4-F-Ph         H   H   H    H   I1379  4-F-Ph       2-Cl-Ph        H   H   H    H   I1380  4-F-Ph       4-Cl-Ph        H   H   H    H   I
                表3(续)实例号  A            B         R   R1  R2 R4 Q   熔点℃1381 4-F-Ph    2，4-F2-Ph    H   H    H    H   I   (泡沫)b1382 4-F-Ph    2，4-Cl2-Ph   H   H    H    H   I1383 2-Cl-Ph   Ph             H   H    H    H   I1384 2-Cl-Ph   2-F-Ph         H   H    H    H   I1385 2-Cl-Ph   4-F-Ph         H   H    H    H   I1386 2-Cl-Ph   2-Cl-Ph        H   H    H    H   I1387 2-Cl-Ph   4-Cl-Ph        H   H    H    H   I1388 2-Cl-Ph   2，4-F2-Ph    H   H    H    H   I1389 2-Cl-Ph   2，4-Cl2-Ph   H   H    H    H   I1390 3-Cl-Ph   Ph             H   H    H    H   I1391 3-Cl-Ph   2-F-Ph         H   H    H    H   I1392 3-Cl-Ph   4-F-Ph         H   H    H    H   I1393 3-Cl-Ph   2-Cl-Ph        H   H    H    H   I1394 3-Cl-Ph   4-Cl-Ph        H   H    H    H   I1395 3-Cl-Ph   2，4-F2-Ph    H   H    H    H   I1396 3-Cl-Ph   2，4-Cl2-Ph   H   H    H    H   I1397 4-Cl-Ph   Ph             H   H    H    H   I1398 4-Cl-Ph   2-F-Ph         H   H    H    H   I1399 4-Cl-Ph   4-F-Ph         H   H    H    H   I1400 4-Cl-Ph   2-Cl-Ph        H   H    H    H   I1401 4-Cl-Ph   4-Cl-Ph        H   H    H    H   I1402 4-Cl-Ph   2，4-F2-Ph    H   H    H    H   I1403 4-Cl-Ph   2，4-Cl2-Ph   H   H    H    H   I1404 2-CF3-Ph Ph             H   H    H    H   I1405 2-CF3-Ph 2-F-Ph         H   H    H    H   I1406 2-CF3-Ph 4-F-Ph         H   H    H    H   I
                表3(续)实例号  A                B           R   R1  R2 R4  Q   熔点℃1407 2-CF3-Ph        2-Cl-Ph       H   H    H    H    I1408 2-CF3-Ph        4-Cl-Ph       H   H    H    H    I1409 2-CF3-Ph        2，4-F2-Ph   H   H    H    H    I1410 2-CF3-Ph        2，4-Cl2-Ph  H   H    H    H    I1411 4-CF3-Ph        Ph            H   H    H    H    I1412 4-CF3-Ph        2-F-Ph        H   H    H    H    I1413 4-CF3-Ph        4-F-Ph        H   H    H    H    I1414 4-CF3-Ph        2-Cl-Ph       H   H    H    H    I1415 4-CF3-Ph        4-Cl-Ph       H   H    H    H    I1416 4-CF3-Ph        2，4-F2-Ph   H   H    H    H    I1417 4-CF3-Ph        2，4-Cl2-Ph  H   H    H    H    I1418 2，4-F2-Ph      Ph            H   H    H    H    I1419 2，4-F2-Ph      2-F-Ph        H   H    H    H    I1420 2，4-F2-Ph      4-F-Ph        H   H    H    H    I1421 2，4-F2-Ph      2-Cl-Ph       H   H    H    H    I1422 2，4-F2-Ph      4-Cl-Ph       H   H    H    H    I1423 2，4-F2-Ph      2，4-F2-Ph   H   H    H    H    I1424 2，4-F2-Ph      2，4-Cl2-Ph  H   H    H    H    I1425 2，4-Cl2-Ph     Ph            H   H    H    H    I1426 2，4-Cl2-Ph     2-F-Ph        H   H    H    H    I1427 2，4-Cl2-Ph     4-F-Ph        H   H    H    H    I1428 2，4-Cl2-Ph     2-Cl-Ph       H   H    H    H    I1429 2，4-Cl2-Ph     4-Cl-Ph       H   H    H    H    I
           表3(续)实例号     A             B         R  R1  R2  R4 Q   熔点℃1430  2，4-Cl2-Ph 2，4-F2-Ph   H   H    H    H    I1431  2，4-Cl2-Ph 2，4-Cl2-Ph  H   H    H    H    I1432  Ph           2，4-F2-Ph   H   H    H    H    -SS-1433  4-F-Ph       2-F-Ph        H   H    H    H    -SS-1434  4-F-Ph       2，4-F2-Ph   H   H    H    H    -SS-1435  Ph           2，4-F2-Ph   H   H    H    H    -SSCH31436  4-F-Ph       2-F-Ph        H   H    H    H    -SSCH31437  4-F-Ph       2，4-F2-Ph   H   H    H    H    -SSCH3
                                                  O
                                                  ″1438  Ph           2，4-F2-Ph   H   H    H    H    SCNHMe
                                                  O
                                                  ″1439  4-F-Ph       2-F-Ph        H   H    H    H    SCNHMe
                                                  O
                                                  ″1440  4-F-Ph       2，4-F2-Ph   H   H    H    H    SCNHMe
                                                  O
                                                  ″1441  Ph           2，4-F2-Ph   H   H    H    H    SCNH-n-Bu
                                                  O
                                                  ″1442  4-F-Ph       2-F-Ph        H   H    H    H    SCNH-n-Bu
                                                  O
                                                  ″1443  4-F-Ph       2，4-F2-Ph   H   H    H    H    SCNH-n-Bu1444  Ph           2，4-F2-Ph   H   H    H    H    Cl1445  4-F-Ph       2-F-Ph        H   H    H    H    Cl1446  4-F-Ph       2，4-F2-Ph   H   H    H    H    Cl1447  Ph           2，4-F2-Ph   H   H    H    H    CHO1448  4-F-Ph       2-F-Ph        H   H    H    H    CHO1449  4-F-Ph       2，4-F2-Ph   H   H    H    H    CHO
        表3(续)实例号    A         B         R   R1  R2  R4  Q       熔点℃1450   Ph        2，4-F2-Ph H   H    H    H    SCH2CN1451   4-F-Ph    2-F-Ph      H   H    H    H    SCH2CN   油c1452   4-F-Ph    2，4-F2-Ph H   H    H    H    SCH2CN1453   Ph        2，4-F2-Ph H   H    H    H    SCH2SCN1454   4-F-Ph    2-F-Ph      H   H    H    H    SCH2SCN1455   4-F-Ph    2，4-F2-Ph H   H    H    H    SCH2SCN1456   Ph        2，4-F2-Ph H   H    H    H    SCCl31457   4-F-Ph    2-F-Ph      H   H    H    H    SCCl31458   4-F-Ph    2，4-F2-Ph H   H    H    H    SCCl31459   Ph        4-F-Ph      H   H    H    H    S-n-Bu    半固体d1460   4-F-Ph    2-F-Ph      H   H    H    H    F1461   4-F-Ph    2-F-Ph      H   H    H    H    Br
                                             O
                                             ″1462   4-F-Ph    2-F-Ph      H   H    H    H    SCH3
                                             O
                                             ″1463   4-F-Ph    2-F-Ph      H   H    H    H    SCH3
                                             ″
                                             O
                                             O
                                             ″1464   4-F-Ph    2-F-Ph      H   H    H    H    S-n-Pr
                                             ″
                                             O
                                             O
                                             ″1465   4-F-Ph    2-F-Ph      H   H    H    H    -S-t-Bu1466   4-F-Ph    2-F-Ph      H   H    H    H    SCF2H1467   4-F-Ph    2-F-Ph      H   H    H    H    SCF2CF2H
                                             O
                                             ″1468* 4-F-Ph    2-F-Ph      H   H    H    H    SCH2CN   (油)e
          表3(续)实例号   A       B      R  R1  R2  R4  Q       熔点℃
                                       O
                                       ″1469*4-F-Ph  2-F-Ph  H   H    H    H     SCH2CN  (油)f
                                       ″
                                       O
                                       O
                                       ″1470  4-F-Ph  2-F-Ph   H   H    H    H    SCH2SCN
                                       ″
                                       O
                                       O CH3
                                       ″′1471  4-F-Ph  2-F-Ph   H   H    H    H    S-CHCN
                                       ″
                                       O
                                       O
                                       ″1472  4-F-Ph  2-F-Ph   H   H    H    H    SCH2CO2CH3
                                       ″
                                       O
                                       O
                                       ″1473  4-F-Ph  2-F-Ph   H   H    H    H    SCNH-allyl
                                       O
                                       ″1474  4-F-Ph  2-F-Ph   H   H    H    H    SCNH-i-Pr
                                       O
                                       ″1475  4-F-Ph  2-F-Ph   H   H    H    H    SCNHPh
                                       O
                                       ″1476  4-F-Ph  2-F-Ph   H   H    H    H    SCNH-(4-Cl-Ph)
                                       O
                                       ″1477  4-F-Ph  2-F-Ph   H   H    H    H    SCNHCH2Ph
                                       O
                                       ″1478  4-F-Ph  2-F-Ph   H   H    H    H    SCNHCH2-(4-CH3O-Ph)
                                       O
                                       ″1479  4-F-Ph  2-F-Ph   H   H    H    H    CCH3
        表3(续)实例号   A         B       R   R1 R2 R4 Q    熔点℃
                                        O
                                        ″1480  4-F-Ph    2-F-Ph    H   H   H   H    COH
                                        O
                                        ″1481  4-F-Ph    2-F-Ph    H   H   H   H    COCH3
                                        O
                                        ″1482  4-F-Ph    2-F-Ph    H   H   H   H    CO-i-Pr1483  4-F-Ph    2-F-Ph    H   H   H   H    SCN1484  4-F-Ph    2-F-Ph    H   H   H   H    SSCH2Ph1485  4-F-Ph    2-F-Ph    H   H   H   H    SS-allyl1486  4-F-Ph    2-F-Ph    H   H   H   H    SSPha NMR：(CDCl3)δ4.9(s，2H)；5.1(s，1H)；5.2(s，1H)；
   5.3(s，1H)；6.7(m，2H)；6.9(m，2H)；7.2(m，2H)；
   7.5(m，1H)；7.6(s，1H)；12.2(brs，1H).b NMR：(CDCl3)δ4.7(ABq，2H)；5.3(s，2H)；5.8(s，
   1H)；6.7(m，2H)；6.9(m，2H)；7.3(m，2H)；7.5(m，
   1H)；7.8(s，1H).c NMR：(CDCl3)δ3.8(ABq，2H)；4.7(ABq，2H)；5.2(s，
   1H)；5.3(two s，2H)；6.9-7.2(m，4H)；7.2-7.4(m，
   3H)；7.5(m，1H)；7.8(s，1H).d NMR：(CDCl3)δ0.92(t，3H)；1.4-1.7(m，4H)；3.1(t，
   2H)；4.5(ABq，2H)；5.4(two s，2H)；5.8(s，1H)；
   7.0(m，4H)；7.2(m，3H)；7.5(m，2H)；7.8(s，1H).e NMR：(CDCl3)δ 2.7-3.5(m，2H)；4.3(s，1H)；4.4(m，
   2H)；5.2(m，2H)；6.8-7.4(m，8H)；7.9(m，1H).f NMR：(CDCl3)δ2.7-3.4(m，2H)；4.2(d，1H)；4.5
   (ABq，2H)；5.3(m，2H)；6.8-7.4(m，8H)；7.9(d，1H).
                           实例14872，3-双(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3，4-环氧-2-丁醇。
把2，3-双(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇(1.0克)溶于50毫升无水苯并在氮气下搅拌。在溶液中加入0.012克丙酮酸钒。然后回流溶液并于10分钟滴加叔丁基氢过氧化物(0.44克溶介于5毫升无水苯中)。反应液再回流1小时，然后冷却至环境温度。真空除去苯，剩余物经硅胶色谱层析(2％MeOH/CH2Cl2)。得总量650毫克比例为3∶1的非对映异构体。进一步色谱法分离非对映异构体。所得的主要异构体为一种蜡状白色固体。NMR(CDCl3/TMS)α2.60(d，J＝6Hz，1H)；3.48(d，J＝6Hz，1H)；4.70(q，J＝7Hz，2H)； 5.25(s，1H)； 6.8-7.3(m，8H)；7.55(s，1H)；7.90(s，1H)。
此小量的异构体为无定形白色固体。NMR(CDCl3/TMS)δ2.55(d，J＝6H，1H)；2.75(d，J ＝6Hz，1H)；4.80(q，J＝7Hz)；5.0(s，1H)；6.85-7.10(m，4H)；7.15-7.45(m，4H)；7.80(s，1H)； 8.05(s，1H)。
表4所列环氧物已用上述实例1487的方法制备或可以制备。
                  表4
Figure C9210593000921
实例号  A         B            n    R   R1  R2 R3  R4 熔点℃1487 4-F-Ph    4-F-Ph         0    H   H    H    H    H   53-551488 4-F-Ph    2，4-Cl2-Ph   0    H   H    H    H    H1489 4-F-Ph    4-Cl-Ph        0    H   H    H    H    H1490 4-F-Ph    2，4-F2-Ph    0    H   H    H    H    H1491 4-F-Ph    4-CF3-Ph      0    H   H    H    H    H1492 4-F-Ph    2-F-Ph         0    H   H    H    H    H1493 4-F-Ph    2-Cl-Ph        0    H   H    H    H    H1494 4-F-Ph    n-C4F9      0    H   H    H    H    H1495 3-F-Ph    4-F-Ph         0    H   H    H    H    H1496 3-F-Ph    2，4-Cl2-Ph   0    H   H    H    H    H1497 3-F-Ph    4-Cl-Ph        0    H   H    H    H    H1498 3-F-Ph    2，4-F2-Ph    0    H   H    H    H    H1499 3-F-Ph    4-CF3-Ph      0    H   H    H    H    H1500 3-F-Ph    2-F-Ph         0    H   H    H    H    H1501 3-F-Ph    2-Cl-Ph        0    H   H    H    H    H1502 3-F-Ph    n-C4F9      0    H   H    H    H    H1503 4-Cl-Ph   4-F-Ph         0    H   H    H    H    H1504 4-Cl-Ph   2，4-Cl2-Ph   0    H   H    H    H    H1505 4-Cl-Ph   4-Cl-Ph        0    H   H    H    H    H1506 4-Cl-Ph   2，4-F2-Ph    0    H   H    H    H    H
              表4(续)实例号  A          B           n    R   R1  R2 R3  R4 熔点℃1507 4-Cl-Ph    4-CF3-Ph     0    H   H    H    H    H1508 4-Cl-Ph    2-F-Ph        0    H   H    H    H    H1509 4-Cl-Ph    2-Cl-Ph       0    H   H    H    H    H1510 4-Cl-Ph    n-C4F9     0    H   H    H    H    H1511 2-Cl-Ph    4-F-Ph        0    H   H    H    H    H1512 2-Cl-Ph    2，4-Cl2-Ph  0    H   H    H    H    H1513 2-Cl-Ph    4-Cl-Ph       0    H   H    H    H    H1514 2-Cl-Ph    2，4-F2-Ph   0    H   H    H    H    H1515 2-Cl-Ph    4-CF3-Ph     0    H   H    H    H    H1516 2-Cl-Ph    2-F-Ph        0    H   H    H    H    H1517 2-Cl-Ph    2-Cl-Ph       0    H   H    H    H    H1518 2-Cl-Ph    n-C4F9     0    H   H    H    H    H1519 3-Cl-Ph    4-F-Ph        0    H   H    H    H    H1520 3-Cl-Ph    2，4-Cl2-Ph  0    H   H    H    H    H1521 3-Cl-Ph    4-Cl-Ph       0    H   H    H    H    H1522 3-Cl-Ph    2，4-F2-Ph   0    H   H    H    H    H1523 3-Cl-Ph    4-CF3-Ph     0    H   H    H    H    H1524 3-Cl-Ph    2-F-Ph        0    H   H    H    H    H1525 3-Cl-Ph    2-Cl-Ph       0    H   H    H    H    H1526 3-Cl-Ph    n-C4F9     0    H   H    H    H    H1527 Ph         4-F-Ph        0    H   H    H    H    H    88-941528 Ph         2，4-Cl2-Ph  0    H   H    H    H    H1529 Ph         4-Cl-Ph       0    H   H    H    H    H1530 Ph         2，4-F2-Ph   0    H   H    H    H    H1531 Ph         4-CF3-Ph     0    H   H    H    H    H
             表4(续)实例号 A               B           n     R     R1  R2  R3 R4 熔点℃1533 Ph            2-Cl-Ph        0     H     H    H    H    H1534 Ph            n-C4F9      0     H     H    H    H    H1535 4-CF3-Ph     4-F-Ph        0     H     H    H    H    H1536 4-CF3-Ph     2，4-Cl2-Ph  0     H     H    H    H    H1537 4-CF3-Ph     4-Cl-Ph       0     H     H    H    H    H1538 4-CF3-Ph     2，4-F2-Ph   0     H     H    H    H    H1539 4-CF3-Ph     4-CF3-Ph     0     H     H    H    H    H1540 4-CF3-Ph     2-F-Ph        0     H     H    H    H    H1541 4-CF3-Ph     2-Cl-Ph       0     H     H    H    H    H1542 4-CF3-Ph     n-C4F9     0     H     H    H    H    H1543 4-Br-Ph       4-F-Ph        0     H     H    H    H    H1544 4-Br-Ph       2，4-Cl2-Ph  0     H     H    H    H    H1545 4-Br-Ph       4-Cl-Ph       0     H     H    H    H    H1546 4-Br-Ph       2，4-F2-Ph   0     H     H    H    H    H1547 4-Br-Ph       4-CF3-Ph     0     H     H    H    H    H1548 4-Br-Ph       2-F-Ph        0     H     H    H    H    H1549 4-Br-Ph       2-Cl-Ph       0     H     H    H    H    H1550 4-Br-Ph       n-C4F9      0     H     H    H    H    H1551 2，4-Cl2-Ph  4-F-Ph        0     H     H    H    H    H1552 2，4-Cl2-Ph  2，4-Cl2-Ph  0     H     H    H    H    H1553 2，4-Cl2-Ph  4-Cl-Ph       0     H     H    H    H    H1554 2，4-Cl2-Ph  2，4-F2-Ph   0     H     H    H    H    H1555 2，4-Cl2-Ph  4-CF3-Ph     0     H     H    H    H    H1556 2，4-Cl2-Ph  2-F-Ph        0     H     H    H    H    H1557 2，4-Cl2-Ph  2-Cl-Ph       0     H     H    H    H    H1558 2，4-Cl2-Ph  n-C4F9     0     H     H    H    H    H
              表4(续)实例号  A           B           n R    R1    R2  R3 R4熔点℃1559 2-F-Ph      4-F-Ph        0 H    H       H    H   H1560 2-F-Ph      2，4-Cl2-Ph  0 H    H       H    H   H1561 2-F-Ph      4-Cl-Ph       0 H    H       H    H   H1562 2-F-Ph      2，4-F2-Ph   0 H    H       H    H   H1563 2-F-Ph      4-CF3-Ph     0 H    H       H    H   H1564 2-F-Ph      2-F-Ph        0 H    H       H    H   H1565 2-F-Ph      2-Cl-Ph       0 H    H       H    H   H1566 2-F-Ph      n-C4F9     0 H    H       H    H   H1567 2，4-F2-Ph 4-F-Ph        0 H    H       H    H   H1568 2，4-F2-Ph 2，4-Cl2-Ph  0 H    H       H    H   H1569 2，4-F2-Ph 4-Cl-Ph       0 H    H       H    H   H1570 2，4-F2-Ph 2，4-F2-Ph   0 H    H       H    H   H1571 2，4-F2-Ph 4-CF3-Ph     0 H    H       H    H   H1572 2，4-F2-Ph 2-F-Ph        0 H    H       H    H   H1573 2，4-F2-Ph 2-Cl-Ph       0 H    H       H    H   H1574 2，4-F2-Ph n-C4F9     0 H    H       H    H   H1575 Ph          4-F-Ph        0 H    CH3    H    H   H1576 Ph          4-F-Ph        0 -(CH2)2-   H    H   H1577 Ph          4-F-Ph        0 CH3 CH3    H    H   H1578 4-F-Ph      4-F-Ph        0 H    CH3    H    H   H1579 4-F-Ph      4-F-Ph        0 -(CH2)2-   H    H   H1580 4-F-Ph      4-F-Ph        0 CH3 CH3    H    H   H1581 4-Cl-Ph     2，4-Cl2-Ph  0 H    CH3    H    H   H
              表4(续)实例号  A           B          n    R       R1     R2  R3  R4熔点℃1582  4-Cl-Ph    2，4-Cl2-Ph  0    -(CH2)2-      H    H    H1583  4-Cl-Ph    2，4-Cl2-Ph  0    CH3  CH3      H    H    H1584  2-Cl-Ph    4-Cl-Ph       0    H      CH3      H    H    H1585  2-Cl-Ph    4-Cl-Ph       0    -(CH2)2-       H    H    H1586  2-Cl-Ph    4-Cl-Ph       0    CH3   CH3      H    H    H1587  4-F-Ph     4-F-Ph        0    H      C2H5    H    H    H1588  4-F-Ph     4-F-Ph        0    H      i-C3H7  H    H    H1589  4-F-Ph     4-F-Ph        0    H      n-C4H9  H    H    H1590  4-F-Ph     4-F-Ph        0    H      Ph         H    H    H1591  4-F-Ph     4-F-Ph        0    H      t-C4H9  H    H    H1592  4-F-Ph     4-F-Ph        0    H      Ph         H    H    H1593  4-F-Ph     4-F-Ph        0    CH3   t-C4H9  H    H    H1594  4-F-Ph     4-F-Ph        0    CH3   Ph         H    H    H1595  4-F-Ph     4-F-Ph        0    -(CH2)3-        H    H    H1596  4-F-Ph     4-F-Ph        0    -(CH2)4-        H    H    H1597  4-F-Ph     4-F-Ph        0    -(CH2)5-        H    H    H1598  4-F-Ph     4-F-Ph        0    -(CH2)6-        H    H    H1599  4-CH3-Ph  4-F-Ph        0    H      CH3       H    H    H1600  4-F-Ph     4-F-Ph        1    H      CH3       H    H    H1601  4-Cl-Ph    4-F-Ph        4    H      CH3       H    H    H1602  n-C4F9  4-F-Ph        0    H      CH3       H    H    H1603  (CH3)2N 4-F-Ph        1    H      CH3       H    H    H
              表4(续)实例号      A          B            n R R1   R2         R3 R4 熔点℃1604 5-Cl-2-噻吩基  4-F-Ph         0 H CH3  H            H   H1605 2-Cl-3-噻吩基  4-F-Ph         0 H CH3  H            H   H1606 1-咪唑基       4-F-Ph         0 H CH3  H            H   H1607 4-F-Ph         4-F-Ph         0 H H     CH3         H   H1608 4-F-Ph         4-F-Ph         0 H H     CH2CH＝CH2 H   H1609 4-F-Ph         4-F-Ph         0 H H     COCH3       H   H1610 4-F-Ph         4-F-Ph         0 H H     CO2CH3     H   H1611 4-CF3O-Ph     4-F-Ph         0 H H     H            H   H1612 2-Cl-Ph        4-Cl-Ph        0 H H     CH3         H   H1613 2-Cl-Ph        4-Cl-Ph        0 H H     CH2CH＝CH2 H   H1614 2-Cl-Ph        4-Cl-Ph        0 H H     COCH3       H   H1615 2-Cl-Ph        4-Cl-Ph        0 H H     CO2CH3     H   H1616 4-Cl-Ph        2，4-Cl2-Ph   0 H H     CH3         H   H1617 4-Cl-Ph        2，4-Cl2-Ph   0 H H     CH2CH＝CH2 H   H1618 4-Cl-Ph        2，4-Cl2-Ph   0 H H     COCH3       H   H1619 4-Cl-Ph        2，4-Cl2-Ph   0 H H     CO2CH3     H   H1620 Ph             4-F-Ph         0 H H     CH3         H   H1621 Ph             4-F-Ph         0 H H     CH2CH＝CH2 H   H1622 Ph             4-F-Ph         0 H H     COCH3       H   H1623 Ph             4-F-Ph         0 H H     CO2CH3     H   H1624 OH             2，4-Cl2-Ph   2 H H     H            H   H1625 OH             2，4-Cl2-Ph   3 H H     H            H   H1626 OH             2，4-Cl2-Ph   4 H H     H            H   H
                表4(续)实例号  A                      B            n   R   R1  R2 R3  R41627 1-咪唑基             2，4-Cl2-Ph     1   H   H    H    H    H1628   ″                 2，4-Cl2-Ph     2   H   H    H    H    H1629   ″                 4-F-Ph           3   H   H    H    H    H1630   ″                 4-F-Ph           4   H   H    H    H    H1631 1H-1，2，4-三唑-1-基 4-F-Ph           1   H   H    H    H    H1632   ″                 4-F-Ph           2   H   H    H    H    H1633   ″                 4-F-Ph           3   H   H    H    H    H1634   ″                 4-F-Ph           4   H   H    H    H    H1635   ″                 2，4-Cl2-Ph     1   H   H    H    H    H1636   Ph                 2，5-F2-Ph      0   H   H    H    H    H1637   Ph                 3-F-Ph           0   H   H    H    H    H1638   Ph                 2，5-Cl2-Ph     0   H   H    H    H    H1639   Ph                 3-Cl-Ph          0   H   H    H    H    H1640   Ph                 4-Br-Ph          0   H   H    H    H    H1641   Ph                 4-I-Ph           0   H   H    H    H    H1642   Ph                 3，4-F2-Ph      0   H   H    H    H    H1643   Ph                 3，4-Cl2-Ph     0   H   H    H    H    H1644   Ph                 2，6-Cl2-Ph     0   H   H    H    H    H1645   Ph                 2-Cl-(4-F)-Ph    0   H   H    H    H    H1646   Ph                 2，4，6-Cl3-Ph  0   H   H    H    H    H1647   Ph                 2-F-(4-Cl)-Ph    0   H   H    H    H    H1648   Ph                 Ph               0   H   H    H    H    H1649   Ph                 4-CH3-Ph        0   H   H    H    H    H1650   Ph                 3-CH3-Ph        0   H   H    H    H    H1651   Ph                 2-CH3-Ph        0   H   H    H    H    H1652   Ph                 2-CF3-Ph        0   H   H    H    H    H1653   Ph                 3-CF3-Ph        0   H   H    H    H    H
               表4(续)实例号A            B            n   R   R1 R2  R3  R4  熔点℃1654 Ph       2-F-(4-CF3)-Ph  0   H   H    H    H    H1655 Ph       4-CH3O-Ph       0   H   H    H    H    H1656 Ph       5-Cl-2-吡啶基    0   H   H    H    H    H1657 Ph       5-Cl-2-噻吩基    0   H   H    H    H    H1658 Ph       2-Cl-3-噻吩基    0   H   H    H    H    H1659 Ph       s-C4H9        0   H   H    H    H    H1660 2-Cl-Ph  2，5-F2-Ph     0   H   H    H    H    H1661 2-Cl-Ph  3-F-Ph          0   H   H    H    H    H1662 2-Cl-Ph  2，5-Cl2-Ph    0   H   H    H    H    H1663 2-Cl-Ph  3-Cl-Ph         0   H   H    H    H    H1664 2-Cl-Ph  4-Br-Ph         0   H   H    H    H    H1665 2-Cl-Ph  4-I-Ph          0   H   H    H    H    H1666 2-Cl-Ph  3，4-F2-Ph     0   H   H    H    H    H1667 2-Cl-Ph  3，4-Cl2-Ph    0   H   H    H    H    H1668 2-Cl-Ph  2，6-Cl2-Ph    0   H   H    H    H    H1669 2-Cl-Ph  2-Cl-(4-F)-Ph   0   H   H    H    H    H1670 2-Cl-Ph  2，4，6-Cl3-Ph 0   H   H    H    H    H1671 2-Cl-Ph  2-F-(4-Cl)-Ph   0   H   H    H    H    H1672 2-Cl-Ph  Ph              0   H   H    H    H    H1673 2-Cl-Ph  4-CH3-Ph       0   H   H    H    H    H1674 2-Cl-Ph  3-CH3-Ph       0   H   H    H    H    H1675 2-Cl-Ph  2-CH3-Ph       0   H   H    H    H    H1676 2-Cl-Ph  2-CF3-Ph       0   H   H    H    H    H1677 2-Cl-Ph  3-CF3-Ph       0   H   H    H    H    H1678 2-Cl-Ph  2-F-(4-CF3)-Ph 0   H   H    H    H    H1679 2-Cl-Ph  4-CH3O-Ph      0   H   H    H    H    H
            表4(续)实例号   A           B               n   R   R1 R2  R3  R4熔点℃1680 2-Cl-Ph    5-Cl-2-吡啶基       0   H   H    H    H    H1681 2-Cl-Ph    5-Cl-2-噻吩基       0   H   H    H    H    H1682 2-Cl-Ph    2-Cl-3-噻吩基       0   H   H    H    H    H1683 3-Cl-Ph    2，5-F2-Ph         0   H   H    H    H    H1684 3-Cl-Ph    2，5-Cl2-Ph        0   H   H    H    H    H1685 4-F-Ph     2，5-F2-Ph         0   H   H    H    H    H1686 4-F-Ph     3-F-Ph              0   H   H    H    H    H1687 4-F-Ph     2，5-Cl2-Ph        0   H   H    H    H    H1688 4-F-Ph     3-Cl-Ph             0   H   H    H    H    H1689 4-F-Ph     4-Br-Ph             0   H   H    H    H    H1690 4-F-Ph     4-I-Ph              0   H   H    H    H    H1691 4-F-Ph     3，4-F2-Ph         0   H   H    H    H    H1692 4-F-Ph     3，4-Cl2-Ph        0   H   H    H    H    H1693 4-F-Ph     2，6-Cl2-Ph        0   H   H    H    H    H1694 4-F-Ph     2-Cl-(4-F)-Ph       0   H   H    H    H    H1695 4-F-Ph     2，4，6-Cl3-Ph     0   H   H    H    H    H1696 4-F-Ph     2-F-(4-Cl)-Ph       0   H   H    H    H    H1697 4-F-Ph     Ph                  0   H   H    H    H    H1698 4-F-Ph     4-CH3-Ph           0   H   H    H    H    H1699 4-F-Ph     3-CH3-Ph           0   H   H    H    H    H1700 4-F-Ph     2-CH3-Ph           0   H   H    H    H    H1701 4-F-Ph     2-CF3-Ph           0   H   H    H    H    H1702 4-F-Ph     3-CF3-Ph           0   H   H    H    H    H1703 4-F-Ph     2-F-(4-CF3)-Ph     0   H   H    H    H    H
              表4(续)实例号  A          B              n   R   R1  R2  R3  R4熔点℃1704 4-F-Ph    4-CH3O-Ph        0   H   H    H    H    H1705 4-F-Ph    5-Cl-2-吡啶基     0   H   H    H    H    H1706 4-F-Ph    2-Cl-3-噻吩基     0   H   H    H    H    H1707 4-F-Ph    5-Cl-2-噻吩基     0   H   H    H    H    H1708 3-F-Ph    2，5-Cl2-Ph      0   H   H    H    H    H1709 3-F-Ph    2，5-F2-Ph       0   H   H    H    H    H1710 4-Cl-Ph   2，5-F2-Ph       0   H   H    H    H    H1711 4-Cl-Ph   3-F-Ph            0   H   H    H    H    H1712 4-Cl-Ph   2，5-Cl2-Ph      0   H   H    H    H    H1713 4-Cl-Ph   3-Cl-Ph           0   H   H    H    H    H1714 4-Cl-Ph   4-Br-Ph           0   H   H    H    H    H1715 4-Cl-Ph   4-I-Ph            0   H   H    H    H    H1716 4-Cl-Ph   3，4-F2-Ph       0   H   H    H    H    H1717 4-Cl-Ph   3，4-Cl2-Ph      0   H   H    H    H    H1718 4-Cl-Ph   2，6-Cl2-Ph      0   H   H    H    H    H1719 4-Cl-Ph   2-Cl-(4-F)-Ph     0   H   H    H    H    H1720 4-Cl-Ph   2，4，6-Cl3-Ph   0   H   H    H    H    H1721 4-Cl-Ph   2-F-(4-Cl)-Ph     0   H   H    H    H    H1722 4-Cl-Ph   Ph                0   H   H    H    H    H1723 4-Cl-Ph   4-CH3-Ph         0   H   H    H    H    H1724 4-Cl-Ph   3-CH3-Ph         0   H   H    H    H    H1725 4-Cl-Ph   2-CH3-Ph         0   H   H    H    H    H1726 4-Cl-Ph   2-CF3-Ph         0   H   H    H    H    H1727 4-Cl-Ph   3-CF3-Ph         0   H   H    H    H    H1728 4-Cl-Ph   2-F-(4-CF3)-Ph   0   H   H    H    H    H1729 4-Cl-Ph   4-CH3O-Ph        0   H   H    H    H    H1730 4-Cl-Ph   5-Cl-2-pyridyl    0   H   H    H    H    H
                   表4(续)实例号    A                B            n   R   R1  R2 R3  R4熔点℃1731 4-Cl-Ph          5-Cl-2-噻吩基    0   H   H    H    H    H1732 4-Cl-Ph          2-Cl-3-噻吩基    0   H   H    H    H    H1733 4-Cl-Ph        
Figure C9210593001021
0   H   H    H    H    H1734 4-Cl-Ph          t-丁基           0   H   H    H    H    H1735 4-Cl-Ph          n-己基           0   H   H    H    H    H1736 4-Cl-Ph          n-庚基           0   H   H    H    H    H1737 4-Cl-Ph          n-辛基           0   H   H    H    H    H1738 4-Cl-Ph          -C6F13         0   H   H    H    H    H1739 4-Cl-Ph          -C8F17         0   H   H    H    H    H1740 4-Cl-Ph          4-吡啶基         0   H   H    H    H    H1741 4-Cl-Ph          2-吡啶基         0   H   H    H    H    H1742 4-Cl-Ph          2-噻吩基         0   H   H    H    H    H1743 4-Cl-Ph          4-n-Bu-Ph        0   H   H    H    H    H1744 4-Cl-Ph          4-n-BuO-Ph       0   H   H    H    H    H1745 4-Cl-Ph          5-CF3-2-吡啶基  0   H   H    H    H    H1746 4-Cl-Ph          5-CH3SO2-2-    0   H   H    H    H    H
                   噻吩基1747 4-C2H5-Ph     4-F-Ph            0   H   H    H    H    H1748 4-(n-BuO)-Ph     4-F-Ph            0   H   H    H    H    H1749 2-CH3SO2-     4-F-PH            0   H   H    H    H    H
  咪唑-1-基1750 5-CH3S-1，2，4- 4-F-Ph            0   H   H    H    H    H
  三唑-1-基1751 -C6F13         4-F-Ph            0   H   H    H    H    H1752 -C8F17         4-F-Ph            0   H   H    H    H    H1753 3-CH3O-Ph       4-F-Ph            0   H   H    H    H    H
         表4(续)实例号  A                   B       n   R   R1  R2  R3  R4熔点℃1754 2-CF3-咪唑-1-基     4-F-Ph    0   H   H    H    H    H1755 4-(i-C3H7O)-Ph     4-F-Ph    0   H   H    H    H    H1756 4-I-Ph                4-F-Ph    0   H   H    H    H    H1757 3，4-F2-Ph           4-F-Ph    0   H   H    H    H    H1758 3，4-Cl2-Ph          4-F-Ph    0   H   H    H    H    H1759 2，6-Cl2-Ph          4-F-Ph    0   H   H    H    H    H1760 2-Cl-(4-F)-Ph         4-F-Ph    0   H   H    H    H    H1761 2，4，6-Cl3-Ph       4-F-Ph    0   H   H    H    H    H1762 4-CH3-Ph             4-F-Ph    0   H   H    H    H    H1763 3-CH3-Ph             4-F-Ph    0   H   H    H    H    H1764 2-CH3-Ph             4-F-Ph    0   H   H    H    H    H1765 2-CF3-Ph             4-F-Ph    0   H   H    H    H    H1766 3-CF3-Ph             4-F-Ph    0   H   H    H    H    H1767 4-CH3O-Ph            4-F-Ph    0   H   H    H    H    H1768 2，3-Cl2-Ph          4-F-Ph    0   H   H    H    H    H1769 3，5-Cl2-Ph          4-F-Ph    0   H   H    H    H    H1770 2，5-Cl2-Ph          4-F-Ph    0   H   H    H    H    H1771 3-Br-Ph               4-F-Ph    0   H   H    H    H    H1772 4-C2H5O-Ph         4-F-Ph    0   H   H    H    H    H1773 2，4-(CH3)2-Ph     4-F-Ph    0   H   H    H    H    H1774 2，4，6-(CH3)3-Ph  4-F-Ph    0   H   H    H    H    H1775 4-Ph-Ph               4-F-Ph    0   H   H    H    H    H1776 5-Cl-2-噻吩基         4-F-Ph    0   H   H    H    H    H1777 2-Cl-3-噻吩基         4-F-Ph    0   H   H    H    H    H
       表4(续)实例号  A                     B           n    R   R1 R2  R3  R4熔点℃1778 1-咪唑基              4-F-Ph         0   H   H    H    H    H1779 1H-1，2，4-三唑-1-基  4-F-Ph         0   H   H    H    H    H1780 2-吡啶基              4-F-Ph         0   H   H    H    H    H1781 5-Cl-2-吡啶基         4-F-Ph         0   H   H    H    H    H1782 3-吡啶基              4-F-Ph         0   H   H    H    H    H1783 4-吡啶基              4-F-Ph         0   H   H    H    H    H1784 n-C4F9             4-F-Ph         0   H   H    H    H    H1785 4-I-Ph                2，4-Cl2-Ph   0   H   H    H    H    H1786 3，4-F2-Ph           2，4-Cl2-Ph   0   H   H    H    H    H1787 3，4-Cl2-Ph          2，4-Cl2-Ph   0   H   H    H    H    H1788 2，6-Cl2-Ph          2，4-Cl2-Ph   0   H   H    H    H    H1789 2-Cl-(4-F)-Ph         2，4-Cl2-Ph   0   H   H    H    H    H1790 2，4，6-Cl3-Ph       2，4-Cl2-Ph   0   H   H    H    H    H1791 4-CH3-Ph             2，4-Cl2-Ph   0   H   H    H    H    H1792 3-CH3-Ph             2，4-Cl2-Ph   0   H   H    H    H    H1793 2-CH3-Ph             2，4-Cl2-Ph   0   H   H    H    H    H1794 2-CF3-Ph             2，4-Cl2-Ph   0   H   H    H    H    H1795 3-CF3-Ph             2，4-Cl2-Ph   0   H   H    H    H    H1796 4-CH3O-Ph            2，4-Cl2-Ph   0   H   H    H    H    H1797 2，3-Cl2-Ph          2，4-Cl2-Ph   0   H   H    H    H    H1798 3，5-Cl2-Ph          2，4-Cl2-Ph   0   H   H    H    H    H1799 2，5-Cl2-Ph          2，4-Cl2-Ph   0   H   H    H    H    H1800 3-Br-Ph               2，4-Cl2-Ph   0   H   H    H    H    H1801 4-C2H5O-Ph         2，4-Cl2-Ph   0   H   H    H    H    H1802 2，4-(CH3)2-Ph     2，4-Cl2-Ph   0   H   H    H    H    H
                 表4(续)实例号    A                     B         n   R   R1  R2 R3  R4  熔点℃1803 2，4，6-(CH3)3-Ph  2，4-Cl2-Ph  0   H   H    H    H    H1804 4-Ph-Ph               2，4-Cl2-Ph  0   H   H    H    H    H1805 5-Cl-2-噻吩基         2，4-Cl2-Ph  0   H   H    H    H    H1806 2-Cl-3-噻吩基         2，4-Cl2-Ph  0   H   H    H    H    H1807 1-咪唑基              2，4-Cl2-Ph  0   H   H    H    H    H1808 1H-1，2，4-三唑-1-基  2，4-Cl2-Ph  0   H   H    H    H    H1809 2-吡啶基              2，4-Cl2-Ph  0   H   H    H    H    H1810 5-Cl-2-吡啶基         2，4-Cl2-Ph  0   H   H    H    H    H1811 3-吡啶基              2，4-Cl2-Ph  0   H   H    H    H    H1812 4-吡啶基              2，4-Cl2-Ph  0   H   H    H    H    H1813 n-C4F9             2，4-Cl2-Ph  0   H   H    H    H    H1814 4-I-Ph                4-Cl-Ph       0   H   H    H    H    H1815 3，4-F2-Ph           4-Cl-Ph       0   H   H    H    H    H1816 3，4-Cl2-Ph          4-Cl-Ph       0   H   H    H    H    H1817 2，6-Cl2-Ph          4-Cl-Ph       0   H   H    H    H    H1818 2-Cl-(4-F)-Ph         4-Cl-Ph       0   H   H    H    H    H1819 2，4，6-Cl3-Ph       4-Cl-Ph       0   H   H    H    H    H1820 4-CH3-Ph             4-Cl-Ph       0   H   H    H    H    H1821 3-CH3-Ph             4-Cl-Ph       0   H   H    H    H    H1822 2-CH3-Ph             4-Cl-Ph       0   H   H    H    H    H1823 2-CF3-Ph             4-Cl-Ph       0   H   H    H    H    H1824 3-CF3-Ph             4-Cl-Ph       0   H   H    H    H    H1825 4-CH3O-Ph            4-Cl-Ph       0   H   H    H    H    H
       表4(续)实例号     A                  B         n   R   R1 R2  R3  R4熔点℃1826 2，3-Cl2-Ph         4-Cl-Ph      0   H   H    H    H    H1827 3，5-Cl2-Ph         4-Cl-Ph      0   H   H    H    H    H1828 2，5-Cl2-Ph         4-Cl-Ph      0   H   H    H    H    H1829 3-Br-Ph              4-Cl-Ph      0   H   H    H    H    H1830 4-EtO-Ph             4-Cl-Ph      0   H   H    H    H    H1831 2，4-(CH3)2-Ph    4-Cl-Ph      0   H   H    H    H    H1832 2，4，6-(CH3)3-Ph 4-Cl-Ph      0   H   H    H    H    H1833 4-Ph-Ph              4-Cl-Ph      0   H   H    H    H    H1834 5-Cl-2-噻吩基        4-Cl-Ph      0   H   H    H    H    H1835 2-Cl-3-″″″        4-Cl-Ph      0   H   H    H    H    H1836 1-咪唑基             4-Cl-Ph      0   H   H    H    H    H1837 1H-1，2，4-三唑-1-基 4-Cl-Ph      0   H   H    H    H    H1838 2-吡啶基             4-Cl-Ph      0   H   H    H    H    H1839 5-Cl-2-吡啶基        4-Cl-Ph      0   H   H    H    H    H1840 3-吡啶基             4-Cl-Ph      0   H   H    H    H    H1841 4- ″″″            4-Cl-Ph      0   H   H    H    H    H1842 n-C4F9            4-Cl-Ph       0   H   H    H    H    H1843 4-I-Ph               2，4-F2-Ph  0   H   H    H    H    H1844 3，4-F2-Ph          2，4-F2-Ph  0   H   H    H    H    H1845 3，4-Cl2-Ph         2，4-F2-Ph  0   H   H    H    H    H1846 2，6-Cl2-Ph         2，4-F2-Ph  0   H   H    H    H    H1847 2-Cl-(4-F)-Ph        2，4-F2-Ph  0   H   H    H    H    H1848 2，4，6-Cl3-Ph      2，4-F2-Ph  0   H   H    H    H    H1849 4-CH3-Ph            2，4-F2-Ph  0   H   H    H    H    H1850 3-CH3-Ph            2，4-F2-Ph  0   H   H    H    H    H
      表4(续)实例号  A                      B          n   R  R1  R2  R3  R4熔点℃1851 2-CH3-Ph             2，4-F2-Ph   0   H   H    H    H    H1852 2-CF3-Ph             2，4-F2-Ph   0   H   H    H    H    H1853 3-CF3-Ph             2，4-F2-Ph   0   H   H    H    H    H1854 4-CH3O-Ph            2，4-F2-Ph   0   H   H    H    H    H1855 2，3-Cl2-Ph          2，4-F2-Ph   0   H   H    H    H    H1856 3，5-Cl2-Ph          2，4-F2-Ph   0   H   H    H    H    H1857 2，5-Cl2-Ph          2，4-F2-Ph   0   H   H    H    H    H1858 3-Br-Ph               2，4-F2-Ph   0   H   H    H    H    H1859 4-C2H50-Ph          2，4-F2-Ph   0   H   H    H    H    H1860 2，4-(CH3)2-Ph      2，4-F2-Ph   0   H   H    H    H    H1861 2，4，6-(CH3)3-Ph   2，4-F2-Ph   0   H   H    H    H    H1862 4-Ph-Ph                2，4-F2-Ph   0   H   H    H    H    H1863 5-Cl-2-噻吩基          2，4-F2-Ph   0   H   H    H    H    H1864 2-Cl-3-噻吩基          2，4-F2-Ph   0   H   H    H    H    H1865 1-咪唑基               2，4-F2-Ph   0   H   H    H    H    H1866 1H-1，2，4-三唑-1-基   2，4-F2-Ph   0   H   H    H    H    H1867 2-吡啶基               2，4-F2-Ph   0   H   H    H    H    H1868 5-Cl-2-吡啶基          2，4-F2-Ph   0   H   H    H    H    H1869 3-吡啶基               2，4-F2-Ph   0   H   H    H    H    H1870 4-″″″               2，4-F2-Ph   0   H   H    H    H    H1871 n-C4F9              2，4-F2-Ph   0   H   H    H    H    H
        表4(续)实例号   A         B           n R R1 R2 R3   R4熔点℃1872  4-F-Ph    4-F-Ph        0 H H    H  CH3   H1873  4-F-Ph    4-F-Ph        0 H H    H  CH3   CH31874  4-F-Ph    4-F-Ph        0 H H    H  F      H1875  4-F-Ph    4-F-Ph        0 H H    H  F      CH31876  4-F-Ph    4-F-Ph        0 H H    H  F      F1877  4-Cl-Ph   2，4-Cl2-Ph  0 H H    H  CH3   H1878  4-Cl-Ph   2，4-Cl2-Ph  0 H H    H  CH3   CH31879  4-Cl-Ph   2，4-Cl2-Ph  0 H H    H  F      H1880  4-Cl-Ph   2，4-Cl2-Ph  0 H H    H  F      CH31881  4-Cl-Ph   2，4-Cl2-Ph  0 H H    H  F      F1882  2-Cl-Ph   4-Cl-Ph       0 H H    H  CH3   H1883  2-Cl-Ph   4-Cl-Ph       0 H H    H  CH3   CH31884  2-Cl-Ph   4-Cl-Ph       0 H H    H  F      H1885  2-Cl-Ph   4-Cl-Ph       0 H H    H  F      CH31886  2-Cl-Ph   4-Cl-Ph       0 H H    H  F      F1887  Ph        4-F-Ph        0 H H    H  CH3   H1888  Ph        4-F-Ph        0 H H    H  CH3   CH31889  Ph        4-F-Ph        0 H H    H  F      H1890  Ph        4-F-Ph        0 H H    H  F      CH31891  Ph        4-F-Ph        0 H H    H  F      F药理效用
体内活性(表5)是用试验化合物抑制酵母和真菌生长的最低抑制浓度(MIC)这个述语来表示。
目标生物体，白色含珠菌ATCC11651和烟典霉ATCC28214被标准规格化至107生物体/毫升这个浓度，并维持在-70℃至使用。把试验化合物溶于二甲亚砜(DMSO)中，和用鹰的最小基础介质(EMEM)肉汤释到200微克/毫升的最终浓度。标准杀真菌剂的溶液在-70℃下贮藏，并如需要可用EMEM稀释。
体内测定是采用微滴定度内汤稀释技术〔L.Polonelli和G.Morace于Myeopatholoqia.86，21-28(1984)和C.Mughes等人于Antimicrob.Ag.和Chemo.25，560-562(1984)〕。试验化合物顺次用EMEM稀释得到从100至0.4微克/毫升的梯度浓度。把合适的套管插入到所需的生物体(1×104生物体/毫升的C乳头状体和5×105生物体/毫升的A.fumiqut-us)和于30℃培养24小时。在光密度等于540微米时，用扫描分当光度计测定真菌生长量(流动_MCC)和测定MIC值，MIC表示化合物抑制生长的最低浓度〔V.Grenta，等人于Antimicrob.Ag.和Chemo.22，151-153(1982)〕。
试验化合物的体内活性是取决于受试验或标准剂感染的动物生存数同受染的未处理组(表6)比较的百分数(％)。该体内测定是在感染后的7天里使老鼠至死的慢性系统感染，〔J.Barnes等人，Lab，Investigat-ion，49，460-467(1963)和T.Rogers和E.Balish，感染和免疫，14，33-38(1976)〕。
用盐水把维持在-70℃的冰冻贮藏培养基白色念真菌ATCC 11651稀释成1×107生物体/毫升和把0.2毫升经静脉(尾部静脉)接种到20.0克CF-1雌鼠(Charles River)。
果没有使用难溶于10％(W/V)Emulophor_(EL620 GAF Corp.)的试标准*验化合物，那些化合物按惯例溶于0.25％(W/V)甲基纤维素(Methocel)。标准杀真菌剂，水中的两性霉素B(Fungizone_)和甲基纤维素的Ketoconazale(Nizoral_)分别为1.0毫克/公斤/天和150毫克/公斤/天给药。
在初级测定中，鼠(组织10只)经C.乳头状体感染，并且用皮下途径，以50或150毫克/公斤/天给试验化合物。动物感染后1和6小时用量试验化合物，然后的三天里一天一次。记录21天内每组鼠的存活数。
14天用量在150毫克/公斤/天或以下能起到防止70％的受染动物的化合物认作为有活性。
        表5
    体内杀真菌结果
Figure C9210593001111
                      MIC值(微克/毫升)实例号                    C.乳头状体  A.fumigatus1                        ≤0.01        6.31 HCl盐                    0.05        12.52                        ≤0.4         1.63                        ≤0.4         504                          0.03        0.86                          1.6         2510                          1.6         2.515                          0.1         5016                          0.03        6.317                          0.03        12.525                          1.6         2526                        ≤0.4         12.526HCl  盐                   0.03        0.427                        ≤0.4         12.528                          0.03        1.632                        ≤0.4         1.633                          0.03        0.0334                          0.03        3.234HCl 盐                    0.03        1.635                          0.03        0.135HCl 盐                    0.03      ≤0.239                          0.4         2540                          0.4         3.2
        表5(续)
                    MIC值(微克/毫升)实例号            C.乳头状体    A.fumigatus
41                 0.4           50
42                 0.03          6.3
47                 0.03          1.6
49                 0.03          12.5
50                 0.1           0.8
51                 0.03          3.2
52                 0.03          0.4
52HCl 盐           0.03          0.4
65                 0.2           100
67                 0.03          100
85               ≤0.4           12.5
94                 0.4           50
99                 0.05          6.3
100                0.03          3.2
101                0.03          12.5
114                0.4           50
117                0.4           100
163                0.03          12.5
164                0.03          1.6
170                1.6           100
177                3.2         ＞100
208                1.6           50
286                0.4           25
291                0.2           100
359                0.4           50
360                0.8           100
361                0.8           25
363                100           100
447                3.2           N.T.
449              ≤0.4           N.T.
                         表5(续)
                MIC值(微克/毫升)
实例号    C.乳头状体     A.fumigatus
450         ＞100           N.T.
451           12.5          N.T.
452         ＞100           N.T.
453           1.6         ＞100
454           100         ＞100
455           25            N.T.
477         ＞100           N.T.
594           0.8           0.8
594HCl盐      0.03          0.4
596           0.05          0.4
603           0.1         ＞100
605           0.2           100
608           0.4           6.3
620           0.03          0.05
622           0.03          0.1
627           0.03          25
644           0.03          0.4
646           0.03          0.4
651           0.8           100
656         ≤0.4           12.5
657           0.4           100
661           1，6          100
667           6.3           25
668           0.4           50
669           0.03          0.8
671           0.03          0.2
675           0.1           25
685           0.8           100
699           50            100
721           0.4           12.5
                表5(续)
             MIC值(微克/毫升)
实例号    C.乳头状体  A.fumigatus
 724         0.4          0.4
 726         0.8          6.3
 815         0.03       ＞100
 905         0.04         100
1258         1.6        ＞100
1260         0.8        ＞100
1276         0.03         1.6
1276a        3.2          100
1277         0.03         6.3
1277HCl 盐   0.03         3.2
1277a        6.3          100
1278       ≤0.4        ＞100
1300       ≤0.4          6.3
1377         1.6          100
1451       ＞100        ＞100
1459       ＞100        ＞100
1487         0.4          6.3
1527         0.4          6.3
两性霉素B   0.33±0.2    1.4±0.5
制霉菌素    1.3±0       3.0±1.0
5-氟胞嘧啶  0.14±0.1    5.7±4.0
Ketoconazole ≤0.1       11.0±5.0
Miconazole   ≤0.1       1.3±0
*标准药物的MIC值为5次测定的平均值，±标准偏差
         表6
体内杀真菌结果
％存活(150毫升/公斤/天)
                天
 实例号   7     14     21
  1      100    100    80
  2      100    100    80
  3      100    100    60
  4      100    50    N.T.没试验
  6      50     10     0
 10      20     10     0
 15      100    90     60
 16      100    100    100
 17      100    90     70
 25      100    100    50
 26      100    100    100
 26盐    100    90     80
 27      100    100    100
 28      100    90     N.T.
 32      100    90     50
 33      100    100    100
 34      100    100    100
 34盐    100    100    100
 35      100    100    90
 35盐    100    100    70
 39      100    80     N.T.
 40      100    100    N.T.
 41      100    100    N.T.
 42      80     80     50
 47      90     80     30
 49      100    90     60
 50      100    90     50
 51      100    100    80
 52      100    100    90
 52盐    100    100    90
 55      100    70     50
 65      100    70     50
 67      100    100    100
 85      100    80     70
 94      100    40     10
 99      100    100    40
100      100    50     30
101      100    90     60
114      70     10     10
117      60     0      0
163      90     60     40
        表6(续)
      体内杀真菌结果
    ％存活(150毫升/公斤/天)
              天
实例号   7      14    21
 164    100     80    70
 208      0      0     0
 286    100     50    20
 359    100     80    80
 360    100     60    40
 361    100    100    90
 363     10      0     0
 453     60     40    30
 594     70     10     0
 596     70     60    40
 603     10      0     0
 608    100     70    20
 620    100    100    90
 622    100    100   100
 627      0      0     0
 644     80     70    50
 646    100    100    70
 651    100     50    20
 656    100     90    40
 657      0      0     0
 661     50     20     0
 667     10      0     0
 668     70     10     0
 669    100    100   100
 671    100    100    60
 675    100     60     0
 685     30     10     0
 721    100     30    30
 724    100     90    40
 725     90     90    40
 726    100     80    10
 905     80     50    20
1276    100     70    50
1276a     0      0     0
1277    100    100    90
1277a    80      0     0
1278      0      0     0
1487    100    100    70
1527    100     70    20
本发明抗真菌剂能够通过活性组分同体内介质的作用位置作用来给药。本化合物用任何常规的方法同药物一起给药，可以作为单独治疗剂或作为一种组合的治疗剂。他们可以单独给药，但通常是同按照所选择的给药途径和标准药物实践所造的药物载体一起给药。
当然，给药剂量将随着使用和所知因素如具体剂和药效特性，剂的形式和给药途径，受体的年龄，健康和体重；症状的性质和程度，同时治疗的类型，治疗的次数以及所期望的效果而变化。
给药的适合剂量形式(组合物)含有每单位约200毫克至约2000毫克的活性组分。在这些药物组合物中，活性组分通常是组分的总量的约0.5-95％(重量)存在的。在用于治疗上述疾病中，每公斤体重的活性组分的每天用量可以约10至50毫克。
本发明组合物可以组成常规的药物，适用于口服给药如片剂，胶囊，乳剂或水或油状溶液或悬浮液，或适用于局部使用如乳膏，软膏或凝胶。也可以用无菌液体剂量形式肠胃外给药。
明胶囊含有活性组分和粉末载体，如乳糖，淀粉，纤维素衍生物，硬脂酸镁，硬脂酸等。能采用类似的稀释剂来压制成片剂。能把片剂和胶囊制成持续稀放的产品，提供在几个小时里持续释放药性。压制片剂可包有糖溶衣或胶溶衣，罩住任何令人不愉快的味道和防护片剂接触大气，或包有肠溶衣在肠胃道中选择性的崩解。
软膏，乳膏和凝胶的药物组合物能够含有例如常见的稀释剂如动物和植物脂肪，蜡，石蜡，淀粉，西黄蓍胶，纤维素衍生物，聚乙二醇，硅氧烷，膨润土，硅酸，滑石和氧化锌或这些物质的混合物。
通常，水，合适的油，盐水，葡萄糖水溶液，相关的糖溶液和二元醇如聚乙二醇或丙二醇的肠胃外溶液的合适载体。肠胃外给药溶液最好含有活性组分的水溶性盐，合适稳定剂，如需要可含缓冲物。抗氧剂如二亚硫酸钠，亚硫酸钠，或抗坏血酸，其可单独或组合都是合适的稳定剂。
本发明的全部药物组合物还可以含着色剂和芳香剂来帮助病人吸收。
还可使用柠檬酸和其盐以及EDTA钠盐。此外，肠胃溶液能含有防腐剂如benzalkonium的氯化物，甲基或丙基一paraben和氯丁醇。
A.Osol.在Remington′s药物科学中描述合适的药物载体，其为本领域的标准参考文献
本发明化合物组药的有效药物剂量形式描述如下：
胶囊
充填标准的二部分组成硬明胶囊来制成大量单元胶囊，每单元其具有100毫克粉状活性组分，150毫克乳糖，50毫克纤维素和6毫克硬脂酸镁。
软明胶囊
制备活性组分的可消化油组合物，可消化油如大豆油，棉子油或橄榄油，以及用正排量泵把混合物注入明胶形成含有100毫克活性组分的软明胶囊。洗涤和干燥胶囊。
片剂
按常规方法制备大量片剂，以得剂量单位为100毫克活性组分，0.2毫克胶态二氧化硅，5毫克硬脂酸镁，275毫克微晶纤维素，11毫克干法和98.8毫克乳糖。用以使用合适的溶衣增加可口性成延迟吸收。
可注射剂
搅拌1.5％(重量)活性组分的10％(体积)丙二醇制得适用注射给药的肠胃外组合物。用水调节溶液至体积用于注射并无菌。
悬浮液
制备口服给药的含水悬浮液，其每5毫升含100毫克磨碎的活性组分，100毫克羧甲纤维素钠，5毫克苯甲酸钠，1.0克山梨醇溶液，U.S.P.，和0.025毫升香草醛。
软膏
用于局部使用的软膏由掺和100毫克粉末活性组分的5克软膏基质来制备，软膏基质含有40％白色矿腊，3％非晶体蜡，10％羊毛脂，5％山梨糖醇酯类，0.3％吐温20和41.7％水。
当本发明化合物用于农业用途时，通常同一种固体或固体稀释剂一起配制成同有机溶剂配制。用常规的方式就能配制式I化合物的有效配方。它们包括粉剂，颗粒，丸，溶液，乳胶，可湿粉末，浓缩乳剂等。其大多数可以直接使用。可喷射配方能推广至适合的介质，喷体积每公顷从约1至几百升。高强度化合物起初用作为进一步配方的中间体。本配方大致可含约1％至99％重量的活性组分和至少含a)约0.1％至35％表面活性剂和b)约5％至99％固体或液体惰性稀释剂的其中之一。具体地说，他们含有下列这些组分的近似比例：
                             重  量  表  示
                 活性组分    稀释剂    表面活性剂
可湿粉末           20-90      0-24        1-10
油悬液，乳胶，溶液 5-50       40-95       0-35
(包括浓缩乳剂)
含水悬浮液         10-50      40-84       1-20
粉剂               1-25       70-99       0-5
颗粒和丸           1-95       5-99        0-15
高强度化合物       90-99      0-10        0-2
当然，活性组分量需存在的低或高取决于其的用途和化合物的物理性质。有时希望对活性组分是高比例的表面活性剂，这可通过掺入配方或罐混合来达到。
Watkins等人在第2版“杀虫粉剂稀释剂和载体手册”(Dorlandbooks，coldwell，新泽西州)上描述典型固体稀释剂。对可湿粉末较好用易吸收稀释剂和较高密度的适合粉剂。Marsden在“溶剂指南”第二版(Interscience，纽约，1950)。悬浮液浓度较好是低于0.1％的溶介质，溶液浓度较好对于0℃抗相分散是较稳定的。“McCutcheon′sDetergrents and Emulsifiers Annual”(Mc出版公司，Ridgewood，新泽西州)以及Sisely和Wood的“表面活性剂百科金书”(化学出版有限公司，纽约，1964年)列举表面活性剂和其用途。所有配方能含有微量添加剂来减少泡沫，结块，腐蚀，微生物生长等。最好用以使用组分是经美国环境保护署批准。
配制这类组分的方法是已知的，简单混合物组分配制溶液。细粒固体组合物用掺合制备和通常于锤或液体能量碾机研磨。用湿研磨制备悬浮液(例如见Litter，美国专利3,060,084)。颗粒和丸用在制成的颗粒载体上喷射活性物质或聚集技术来制备。参见J.E.Browning“聚集作用”《化学工程》1967年10月4日pp.147ff和“Perry′s化学工程师手册”第四版本，McGraw-Hill，N.Y.1963，pp.8-59ff。
关于配制技术的进一步资料可见下列：
H.M.Loux，1966年2月15日的美国专利3,235,361号，Col.6 16行至Vol.719行和实例10至41。
R.W.Luckenbaugh，1967年3月14日的美国专利3,309,192号Col.543行至Col，762行和实例8，12，15，39，41，52，53，58，132，138-140，162-164，166，167，169-182。
H.Gysin和E.Knusli，1959年6月23日的美国专利2,891,855号Col.366行至Col.517行和实例1-4。
G.C.Klingman，“控制杂草科学”(Weed Control as a Science)John Wiley and Sons，Inc.，纽约，1961，pp.81-96。
J.D.Fryer和S.A.Evans，“控制杂草手册”(Weed ControlHandbool”第5版本，布莱克韦尔科学出版社，牛津，1968，pp101-103。
本发明化合物有效配方的实例如下：
可湿粉末
2-(2，4-二氟苯基)-3-(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-1-醇，和其(S)对映体 80％
烷基苯磺酸钠         2％
木素磺酸钠           2％
人造非晶形硅石       3％
高岭土               13％
组分用掺合，锤研磨，再掺合和包装。
颗粒
上例可湿粉末         15％
石膏                 18％
硫酸钾               16％
在旋转或流化床混合器中掺合组合，并且喷射水使达到成颗粒作用。当大多数物质达到1.0到0.42毫米的理想范围(美国标准号18到40筛眼)，移去，干燥和骤冷颗粒。捣碎过筛物质形成理想范围的增加物。
高强度浓度
2-(2-氟苯基)-3-(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体  98.5％
硅补强剂          0.5％
人造非晶形硅石    1.0％
组分经掺合和于锤-研磨机里捣碎，产生一种高强度浓度，其基本上都通过美国标准号50筛(0.3毫米孔)。然后该物质可以各种方式来配制。
含水悬液
2-(2，4-二氟苯基)-3-苯基-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体    25％
水合硅镁土      3％
粗木素磺酸钙    10％
磷酸二氢钠      0.5％
水              61.5％
在一个球或滚柱研磨机里；组分同砂一起捣碎至固体粒子直径达到10微米以下。
溶液
2-(2，4-二氟苯基)-3-(4-氯苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体    30％
二甲基甲酰胺            70％
合并和搅拌组分得到一溶液，其能被用作于低体积应用。
浓缩乳剂
2-(2，4-二氟苯基)-3-(4-氟苯基)-1-(1H-1，2，4-三唑-1-基)-3-丁烯-2-醇；和其(S)对映体             15％
掺合的磺酸钙和非离子表面活性剂   25％
二甲苯                           60％
合并和搅拌组分直至活性组分全溶介在包装操作中包括精细筛滤板，保障产品里不含有外来不溶性物质。
本发明化合物能有效地用作为植物疾病控制剂，他们有被控制广谱植物疾症，尤其装饰物的植物病原体，蔬菜，田地，谷类和水果作物，例如柄锈属recondita，白粉菌属cichoracearum，白粉菌属graminis，黑星属inaequalis，尾孢菌属arachidicola，和Monilinia fructicola，丝核菌属solani，Pyricularia qzyzae，葡萄孢属cinerea，Pseudocerco-sprorella.herpotrichloride和Cercosporidium personatum.他们也能控制种子病原体。
通常，疾病控制是借助于把有效量的本化合物预感或后感染的施于需保护的植物部分来完成的，如施于根部，茎，叶，水果，种子，块茎或球根，或需保护植物所生长的介质(土壤或沙)。也可把化合物施于利子，也就保护了的生长植物。
众多环境因素能影响这些化合物的施用比率，并且应由实标使用条件来决定。通常叶子用从小于1克/公顷至5000克/顷活性组分的比率就能得到保护。用从0.1至约20公斤/公顷浓度处理生长于土壤的植物就能防治疾病。种子和幼苗一般每公斤种子用从0.06至约3克的比率处理起到保护。
为了获得理想的结果，即少费时，费力和物质，把本发明化合物同杀真菌剂，杀菌剂，杀螨剂，杀线虫剂，杀虫药剂或其它生物活性化合物混合。这些生物活性物质的每份加入量对于本发明组合物来说明可以从0.05至25份重量。这利类型的合适试剂是本领域技术人员熟知的。其中一些列于如下：
杀  真  菌  剂2-苯并咪唑氨基甲酸甲酯(Carfendazim)四甲基二硫化四烷基秋兰姆(秋兰姆)n-十二烷基乙酸胍(dodine)亚乙基双二硫代氨基甲酸锰(maneb)1，4-二氯-2，5-二甲氧基苯(Chloroneb)1-(丁基氨基甲酰基)-2-苯并咪唑氨基甲酸甲酯(benomyl)2-氰基-N-乙基氨基甲酰基)-2-甲氧基亚氨基乙酰胺(Cymoxanil)N-三氯甲硫基四氢邻苯二酰胺(captan)N-三氯甲硫基邻苯二酰胺(folpet)4，4′-(邻亚苯基)双(3-硫代脲基甲酸)二酯(硫代phanate-甲基)2-(噻唑-4-基)苯并咪唑(thiabendazole)三(邻乙基膦酸)(phos乙基铝)四氯异邻苯二甲腈三铝(Chlorothalon-il)2，6-二氯-4-硝基苯胺(dichloran)N-(2，6-二甲苯基)-N-(甲氧乙酰基)苯胺甲酯(metalaxyl)顺-N-〔(1，1，2，2-四氯乙基)硫代〕环己烯-4-1，2-dicarbioximide(Captafol)3-(3，5-二氯苯基)-N-(1-甲乙基)-2，4-二氧代-1-咪唑烷羰基酰胺(ipzodione)3-(3，5-二氯苯基)-5-乙烯基-5-甲基-2，4-唑烷二酮(Vinclozolin)春日霉素O-乙基-S，S-二苯基二硫代磷酸酯(edifenphos)4-(3-(4-(1，1-二甲基-乙基)苯基)-2-甲基)丙基-2，6-二甲基吗啉(Fenpzopimorph)
              杀菌剂三元硫酸铜链霉素硫酸酯土霉素
             杀螨剂异戊烯酸(2-仲丁基-4，6-二硝基苯酚酯(binapacryl)6-甲-1，3-二硫酚并〔2，3-B〕喹啉-2-酮(Oxythioquinox)2，2，2-三氯-1，1-双(4-氯苯基)乙醇(dicofol)双(五氯-2，4-环戊二烯-1-基)(二烯醇氯)三环己基己基氢氧化锡(Cyhexatin)hexakis(2-甲基-2-苯丙基)二锡噁烷(fenvutinqxide)
            杀  线  虫  剂2-〔二乙氧基氧膦基亚胺-1，3-二ethietane(fosthietan)S-甲基-1-(二甲基氨基甲酰基)-N-(甲基氨基甲酰氧基)硫代亚胺甲基酯(oxamyl)S-甲基-1-氨基甲酰基)-N-(甲基氨基甲酰氧基)硫代亚胺甲基酯N-异丙基氨基磷酸O-乙基-O′-〔4-(甲硫基)一间甲苯基〕二酯(fena-mipnos)
               杀虫药剂3-羟基-N-甲基丁烯酰胺(二甲基磷酸)酯(monocrotophos)甲基氨基甲酸2，3-二氢-2，2-二甲基-7-苯并呋喃醇酯(Carbofuran)O-〔2，4，5-三氯-α-(氯甲基)苯基〕磷酸O；O，一二甲基酯(tetrachlorvinphos)2-巯基磷酸二甲酯(malathion)二硫代磷酸O.O-二甲基，O-对硝基苯基酯(甲基对硫磷)甲基氨基甲酸α-苯酚酯(carbarrt)N-〔〔(甲胺基)羰基〕氧基〕硫代乙亚胺酸甲酯(methomyl)N′-(4-氯-邻甲苯)-N，N-二甲基甲脒(chlordimeform)O，O-二乙基-O-(2-异丙基-4-甲基-6-嘧啶基)硫代磷酸(diazinOn)辛氯烯(toxaphene)O-对硝基苯基苯基硫代磷酸O-乙酯(EPN)4-氯-α-(1-甲乙基)苯乙酸氰基(3-苯氧基苯)甲酯(fenvalerate)(±)-顺，反-3-(2，2-二氯乙基)-2，2-二甲基环戊羧酸(3-苯氧基苯基)甲酯(permethrin)N，N′-〔硫双(N-甲基immo)碳酰氧基〕〕双〔硫代乙亚胺酯〕二甲酯(thiodicarb)phosphorothiolothionic酸O-乙基-O-4-(甲硫基)苯基〕-S-正丙基酯(sulprofos)3-(2，2-二氯乙烯基)-2，2-二甲基环戊烷羧酸α-氰基-3-苯氧基苯苄酯(cypermethrin)4-(二氟甲氧基)-α-(甲乙基)苯基乙酸氰基(3-苯氧基苯基)甲酯(flucythrinate)O，O-二乙基-O-(3，5，6-三氯-2-吡啶基)硫代硫酸酯(chlorpyrifos)O，O-二甲基-s-(4-氧代-1，2，3-苯并三嗪-3-(4H)-基)甲基〕二硫磷酸酯(azinphos-甲基)氨基甲酸酯5，6-二甲基-2-二甲氨基-4-嘧啶基二甲酯(pirimicarb)S-(N-甲酰基-N-甲基氨基甲酰基甲基)-O，O-二甲基二硫磷酸酯(form-othion)S-2-(乙硫基乙基)-O，O-二甲基硫磷酸酯(demeton-S-甲基)顺-3-(2，2-二溴乙烯基)-2，2-二甲基环戊烷酸α-氰基-3-苯氧基苯酯(deltamethrin)N-(2-氯-4-三氟甲苯基)丙氨酸氰基(3-苯氧基苯基)甲酯(fluval-inate)
下面将进一步阐述本发明
                      实例A
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮在含有250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的萃果苗圃上，次日，用能造成萃果疤痕的介质，Venturia inaequalis)(黑星菌属inaepualis)孢子悬浮液接种到植物上，然后置于饱和湿润的房内，在20℃孵化24小时，再置于生长房内，在22℃维持11天，此时进行疾病测定。
                   实例B
取试验化物溶于丙酮中，其用量等于最终体积的6％，再悬浮在含有250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的花生苗圃上。次日，用能造成花生后期叶斑病的介质，Cercosporidium Personatum孢子悬浮液接种到植物上，然后置于饱和湿润房内，在22℃孵化24小时，再置于高湿润房内，在27℃孵化7天，置于生长房内，在29℃维持7天，此时进行疾病测定。
                  实例C
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮在含有250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的大豆苗圃上，次日，用能造成大豆灰霉菌的介质，Botrytis cinerea(葡萄孢属灰质)孢子悬浮液接种到植物上，置于饱和湿润房内，在20℃孵化24小时。此时进行疾病测定。
                   实例D
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮于含有250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的小麦苗圃上，次日，用能造成小麦白粉病的介质，Erysiphe gzaminis f.sp.tritici，(白粉菌属gzaminis f.sp.tritici)孢子粉剂，接种到植物上，置于生长房，在20℃维持6天，此时进行疾病测定。
                  实例E
取试验化合物溶于丙酮中，其量等于最终体积的6％，再悬浮于含有250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷液射到叙述的稻谷苗圃上，次日，用能造成稻谷损害的介质，Pyricularia oryzae(Pyricularia稻属)孢子悬浮液，接种到植物上，置于孢和湿润房内，在270℃孵化24小时，置于生长房，在29℃维持4天，此时进行疾病测定。
                      实例F
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮于含250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的稻谷苗圃上，次日，用能造成稻谷外壳枯萎的介质，Rhizotonia Solani(丝核菌属solahi)孢子悬浮液，接种到植物上，置于孢和湿润房内，在27℃孵化48小时。置于生长房，在29℃维持4天，此时进行疾病测定。
                    实例G
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮于含250ppm表面活性剂TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的小麦苗圃上，次日，用能造成小麦叶锈病的介质，Puccinia recohdita(柄锈属recondita)孢子悬浮液，接种到植物上，置于饱和湿润房内，在20℃孵化24小时，置于生长房，在20℃维持8天，此时进行疾病测定。
                  实例H
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮于含250ppm表面活性剂(TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的蕃茄苗圃上，次日，用能造成蕃茄后期枯萎的介质，Phytophthora infestans(疫霉属infestans)孢子悬浮液，接种到植物上，置于饱和湿润房内，在20℃孵化24小时，置于生长房内，在20℃维持5天，此时进行疾病测定。
                        实例I
取试验化合物溶于丙酮中，其用量等于最终体积的6％，再悬浮于含有250ppm表面活性剂(TREMO14(聚羟醇酯)，浓度为100或20ppm的纯水中。将该悬浮液喷射到叙述的葡萄苗圃上，次日，用能造成葡萄绒毛霉的介质，Plasmorpara viticola(单轴霉属viticola)接种到植物上，置于饱和湿润房内，在20℃孵化24小时，此时进行疾病测定。
                        实例J
取试验化合物溶于丙酮中，使得到的浓度为每毫升0.5公斤/公顷，然后将其加到在罐中的黄瓜种籽土壤里，将种籽和土壤与沙、谷类和Pythium aphanadermatum(腐霉属aphanadermatum)真菌菌丝体的混合物一起接种，造成黄瓜猝倒病，再于生长房内，在30℃孵化14天，此时进行疾病测定。
                      实例K
取试验化合物溶于丙酮中，使得到的溶液浓度为每毫升0.5公斤/公顷，然后将其加到在罐中的棉花种籽和在壤里，将种籽和土壤与沙、谷类和能造成棉花枯萎的介质Rhizoctonia solani(丝核菌属solani)真菌菌丝体的混合物一起接种，并置于在生长房内，在30℃孵化14天，此时进行疾病测定。
                        实例L
取试验化合物溶于丙酮中，使得到的溶液浓度为每毫升0.5公斤/公顷，然后将其加到罐中的黄瓜种籽和土壤里，将种籽和土壤与沙、谷类和能造成黄瓜枯萎的介质Fusarium oxyspoyumf.sp.cucumerinum的真菌菌丝体混合物一起接种，并在生长房内，于30℃孵化14天，此时进行疾病测定。
                    实例M
取试验化合物溶于丙酮中，使得到的溶液浓度为每毫升0.5公斤/公顷，将其加到罐中的马豆种籽和土壤里，再把种籽和土壤与沙、谷类及能造成豆类向南枯萎的介质Sclerotium rolfsii(小菌核属rolfsii)真菌菌丝体混合物一起接种，并置于生长房内，在30℃维持14天，此时再进行疾病测定。
实例A-M的结果列于表7。在表7。在表中，测定数100表示100％控制疾病，测定数0表示有关对照物没有控制疾病。—表示对该化合物没有进行试验。P表示由于植物毒性而没有测定疾病控制。
                        表7实  比    例  例  例  例   例   例  例    例  例  比    例   例   例   例例  率    A   B   C   D    E    F   G     H   I   率    J    K    L    M号(ppm)                                         (Kg/ha)1   100   62 100  81  98   90   97 100    0  12    5    0    P    0    P2   100   62 100  93  98   95  100 100    0  99    5    0    P    0    P3   100  100 100  93  93    5   93 100    0   0    5    0    0    P    P4   100  100 100  88 100   96  100 100    0  81    5    0    0    P    06   100    0  82  84  98    0    0  96   23   0    5    0    0    P    010   100    0  76  52  63    0   17  64    0   0    5    0    0    0    015   100  100 100  99 100    1   93 100   26   0    5    0    P    0    P16   100    -   -  46   -    0    0   -    0  23    5    0    0    P    0
   20   74  99  27  67    0    0 100    -   -17   100    -   -  89   -    0   81   -    0  42    5    0    0    P    0
   20   80 100  57  95    0    0 100    -   -25   100  100 100  96  91   31   48  97    0   0    5    0    P    P   3526   100  100 100  96  86   31   61  97   23  86    5    0   25   25   3527   100   62 100  88  98   95  100 100   24  84    5    0    0    0    028   100   89 100  88  98   81  100 100    0   6    5    0    0    0    032   100  100 100  98  95   97   33 100    0  98    5    0    0    P    P33   100    -   -  56   -    0   60   -    0  24    5    0    0    0    0
   20   47  99  37  89    0   29 100    -   -34   100   69 100  94  60   86   16  66    0   0    5    0    0    0    035   100  100 100  96 100    0  100  96    0  26    5    0    0    0    039   100   89  97  96  98    7  100 100    0  81    5    0    0    0    040   100   19 100  80  91    7   61  96    0   0    5    0    0    0    041   100  100 100  96  98    7   97 100    0 100    5    0    0    0    042   100    -   - 100 100   31   41   -    0  23    5    -    -    -    -
   20   29 100  38  98   15    0 100    -   -47   100    -   -  89   -   31   47   -    0  25    5    -    -    -    -
   20   93 100  26  98   15    0 100    -   -49   100   89 100  62 100   76   96 100    0   0    5    0    P    0    P50   100  100 100  98  95   86   93 100    0  46    5    0    P    0    P51   100  100 100  96 100    0  100 100    0   0    5    P    P    P    P52   100  100 100  95  94   93   81 100    0   0    5    0    P    0    0
                           表7实    比    例   例  例  例  例  例  例  例   例   比    例  例   例   例例    率    A    B   C   D   E   F   G   H     I   率    J    K    L    M号  (ppm)                                        (Kg/ha)65    100   34   96  94  85  30  62 100   0    0    5    0    0    0    067    100    -    -  75   -   0  68   -   2    1    5    0    0    0    0
     20   58   99  60  85   0  35  89   -    -94    100   86   61  96  98  78  36 100   0    0    5    0    0    P    P99    100  100  100  89  83  98  61 100   0   83    5    0    0    P    P100    100  100  100  96  83  95  80 100   0   83    5    P    0    P    0101    100  100  100  94  83   0  80 100   0  100    5    0    0    P    0163    100    -    -  95   -   5   0   -   0    0    5    -    -    -    -
     20    0   81  58  23   5   0  99   -    -164    100    -    -  84   -  15   0   -   8    0    5    -    -    -    -
     20   82  100  57  88   5   0 100   -    -170    100    -    -  20   -  10   0   -   0    0    5    -    -    -    -
     20   19   69  32  95   0   0 100   -    -177    100    -    -  26   -  10   0   -   0    0    5    -    -    -    -
     20   82   26  50  46   0   0 100   -    -208    100   84   37  83  76   4  61  97   0   74    5    0    0    0    0291    100    -    -  81   -   1   0   -  24   78    5    -    -    -    -
     20   32   26   6  83   1   0  73   -    -359    100   72  100  83  95  88  62 100        0    5    0    0    0    0360    100   88  100  71  86  74  49  93        0    5    0    0    0    0361    100    -    -  46   -   1   0   -   2    9    5    -    -    -    -
     20   43   26  29  33   1   0 100   -    -363    100    0   49  92  28   0   0  38   0    0    5    0    0    0    0447    100    -    0  24  46  46   0  30   0   24    5    0    0    0    0448    100    -    0  54   -   0  42  16   0    0    5    -    -    -    -449    100   71    0  24   0  76  13  30   0   51    5    0    0    0    0450    100    -    0  54  11  46  34  30   0   51    5    0    0    0    0451    100   16  100  72   0   0   0   0   0    0    5    0    0    0    0452    100   36    0  54  46   0  67  30   0    0    5    0    0    0    0453    100   55   32  75  94   0   0 100   0    0    5    0    0    0    0
                          表7实  比     例   例  例  例   例    例  例    例   例  比   例    例  例    例例  率     A    B   C   D    E     F   G     H    I   率    J    K    L    M号 (ppm)                                             (Kg/ha)454 100     0    0   0  22    0    0    0    0    0    5    -    -    -    -455 100    64   65   0  12    0    0   43    0    0    5    0    0    0    0456 100    82    0  58  53   98    0   96    9    0    5    0    0    0    0477 100    95  100  76 100   48   48  100    0    0    5    P    P    P    P594 100    86  100  93  77    2    -  100    0   79    5    0   60  100   50596 100     -    -  89   -    0    0    -    0   25    5    -    -    -    -
 20    91   95  35  94    0    0  100    -    -603 100    44   97  91  69    0    -   95    0    0    5    0    0    0    0605 100    70   99  32  81    0    -  100    0    0    5    0    0    0    0608 100    87  100  98  98    4   81  100    0    0    5    0    0    P    P618 100   100  100  98  89    0    -  100    0    0    5    0   80   80    P620 100   100  100  96  98   51  100  100    0    0    5    0    0    P    0622 100   100  100  84  99    0  100  100    0   26    5    0    0    P    0627 100     -    -  38   -    0   14    -    0   61    5    -    -    -    -
 20    31   70  19  81    0    0   99    -    -644 100   100  100  94 100  100  100  100   23    0    5    0    0    P    P646 100   100  100  95  98   97   61  100    0   99    5  100    0    0    0651 100     -    -  42   -    0   62    -    0   46    5    0    0    0    0
 20    67    0   7  67    0    0  100    -    -656 100    93  100  88  97    0   50  100    0   20    5    0    P    P    P657 100    62  100  81  98   49   97  100   24   37    5    0    0    0    0661 100     -    -  56   -    0   70    -    5   85    5    -    -    -    -
 20    81   79  61  62    0   10  100    -    -663 100    42  100  95  99   57   36  100    0   39    5    -    -    -    -667 100     -    -   4   -    0    0    -    0   10    5    0    0    0    0
 20    13   14   7  39    0    0    0    -    -668 100     -    -  76   -    1    0    -   22   31    5    -    -    -    -
 20    65   17  31  31    1    0  100    -    -669 100   100  100  90 100   96  100  100    0    0    5    0    0    P    0671 100   100  100  92  94   84  100  100    0   84    5    0    P    P    0
                    表7实    比   例   例   例  例   例   例  例  例  例   比   例   例  例   例例    率   A    B    C   D    E    F   G   H   I    率   J    K    L    M号(ppm)                                            (Kg/ha)675   100   -    -   30   -    0   62   -   0  69    5   -    -    -    -
     20  40    0   42  44    0    0  16   -   -685   100   -    -    0   -    0   29   -   -   -    5   -    -    -    -
     20  57   66   28  67    -   15 100   -   -721   100  73   89   95  94   18  100 100   0   0    5   P    P    P    P724   100 100  100   95 100   63  100 100   0   0    5   0    P    P    P726   100   -    -    -   -    0    0   -   0  38    5   0   20    0    0
     20  75    0   23  81    0    0 100   -   -815   100  40   98    0  62    2    -  97   0  65    5   0    0    0    0905   100   -    -   19   -    0   37   -   0  87    5   0    0    0    0
     20   7    0   15  47    0    0  16   -   -1276  100 100    -   96 100    1   97 100   0   0    5   0    P    0    P
     20  93  100   86 100    1   52 100   -   -1276a 100   -    -   53   -    1    0   -  16  22    5   -    -    -    -
20   42  26   33   88   1    0  100   -   -1277  100   9   65    0   0    0    0  39   0  25    5   0    0    0    01277a 100   -    -   36   -    1   52   -   8  31    5   -    -    -    -
20   58  74   24   95   1    0  100   -   -1278  100  100 100   87  85   17   36 100   0  16    5   0    0    0    01300  100  100 100   93  92   58   81 100   0   0    5   0    0    0    01304  100  100 100   97 100   78   88 100   0  18    5   0    0    0    01377  100  100 100   96  92   58  100 100   0  44    5   0    P    0    P1381  100  100 100   97  98   51   73 100   0  78    5   0   50    0    01451  100   86  84   48  77    2    -  93   0  79    5   0    0    0    01459  100   72  70   65  31   17    0  65   0  74    5   0    0    0    01468  100   40   0    0  77    2    -  93   0  46    5   0   60    0    01469  100   68  84   81  77    2    - 100  24  89    5   0   80   70    01527  100    0 100   93 100    -   35 100   0   0    5   0    P    0    P

Claims (3)

1.一种制备式(I)化合物或其药物或农业上适宜的盐的方法，
Figure C9210593000021
式中
E为单键或氧原子；
A为N(CH3)2；OH；萘基，有1-2个取代基任意取代的苯基，所述取代基独立地选自CF3、卤素、1-4个碳原子的烷基和OCH3，并且其中不多于一个的基团选自S(O)mR5和吡啶基，
B是1-4个碳原子的烷基；联苯基；1-2个取代基任意取代的苯基，每个取代基独立地选自卤素、甲基、卤代甲基、甲氧基和CF3；或被1或2个卤原子任意取代的2-噻吩基、3-噻吩基和4-吡啶基的杂环；
Q是H；
n为0-1；
每个m各自为0、1或2；
R和R1分别是H、甲基或苯基；R2为H、烯丙基、甲基、 R3和R4各自为H或F；R5是甲基；R7甲基；
R8和R9各自为H或1-4个碳原子的烷基；
该方法包括：
a)当E为单键、R2和Q为H、且R3和R4不为F时，在极性非质子传递溶剂中使以下式II和/或IIa的化合物与式III的化合物反应，得到其中E为单健、R2和Q为H及R3和R4不为F的式(I)化合物，
Figure C9210593000031
其中A、B、R、R1、R2、R3、R4和n如上所限定，但R3和R4不为F，以及X为Br、Cl或I，M是H或金属原子；
b).当E为氧原子时，用适当的环氧化试剂在催化剂存在下，氧化下式化合物，得到其中E为氧原子的式(I)化合物，
Figure C9210593000032
式中A、B、R、R1、R2、R3、R4和n如上所定义。
2.根据权利要求1的方法，其中式(II)和/或(IIa)化合物的制备方法包括：在惰性溶剂中使下式III化合物
Figure C9210593000041
式中M是MgX或Li，X是Cl、Br或I，A、R、R1和n如权
利要求1中所定义，与下式(IV)的卤代酮反应
Figure C9210593000042
式中X是Br或Cl，和B、R3和R4如权利要求1中所定义。
3.根据权利要求1的方法，其中式(II)化合物的制备方法包括：在惰性溶剂中使下式V化合物
Figure C9210593000043
式中A、B、R3和R4和n如权利要求中所定义，与下式化合物反应
       (C6H5)3P＝CRR′式中R和R1如权利要求1中所定义。
CN92105930A 1986-06-23 1992-07-18 杀真菌原醇的制备方法 Expired - Fee Related CN1037514C (zh)

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