CN1628095A - 二胺衍生物,二胺衍生物的制备方法,以及含有二胺衍生物作为活性成分的杀菌剂 - Google Patents
二胺衍生物,二胺衍生物的制备方法,以及含有二胺衍生物作为活性成分的杀菌剂 Download PDFInfo
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Abstract
提供一种杀菌剂,其应用以下通式(1)表示的二胺
衍生物作为活性成分,其中,R1到R7代表特殊的取代基,例
如具有1到6个碳原子的烷基,R8代表可被取代的芳基,或
可被取代的杂芳基。
Description
技术领域
本发明涉及新型二胺衍生物,二胺衍生物的制备方法,以及含有二胺衍生物作为活性成分的杀菌剂。
背景技术
害虫控制在水稻栽培中扮演着重要的角色,特别是各种杀菌剂被开发出并用于对付被认为是一种严重病害的稻瘟病。但是,在期望的杀菌活性以及对有用农作物的不良影响的控制方面,这些杀菌剂并不是总令人满意。另外,近几年,由于农业和园艺杀菌剂的频繁使用,出现了具有抗药性的霉菌,而且现有的杀菌剂并不总是显示出令人满意的杀菌活性。而且,从环境角度考虑,需要提供一种安全并且可以在低浓度下控制有害霉菌的新型杀菌剂。
发明内容
因此,本发明的目的之一在于提供二胺衍生物,其对于控制稻瘟病显示出优异的效果,却不会伤害有用农作物。
为了解决上述的问题,发明者们合成了各种新型二胺衍生物,并且进行了各项与它们的杀菌性能等相关的研究。最后发现了对稻瘟病的控制具有优异效果却不会伤害有用农作物的二胺衍生物,从而完成了本发明。
具体地,本发明包括以下具体内容:
[1]二胺衍生物,其由以下通式(1)表示:
其中,R1代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基;
R2和R7独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的芳基或酰基;
R3和R4独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基或包括结合碳原子在内的具有3到6个碳原子的的环烷基;
R5和R6独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基或可被取代的芳基;排除以下情况,即R3、R4、R5和R6都代表氢原子,或当R3、R4、R5和R6中的任何一个代表可被取代的甲基时,其他的代表氢原子;并且
R8代表可被取代的芳基或可被取代的杂芳基。
[2]根据上述部分[1]的二胺衍生物,其中,
R1代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基,具有2到6个碳原子的链烯基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基;
R2和R7独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基、可被取代的芳基或酰基;
R3和R4独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基或包括结合碳原子在内具有3到6个碳原子的的环烷基;
R5和R6独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基或可被取代的芳基;排除以下情况,即R3、R4、R5和R6都代表氢原子,或当R3、R4、R5和R6中的任何一个代表可被取代的甲基时,其他的代表氢原子。
[3]根据上述部分[2]的二胺衍生物,其中
R2和R7独立地代表氢原子、具有1到6个碳原子的烷基或酰基;
R3和R4独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基、可被取代的芳基或包括结合碳原子在内具有3到6个碳原子的的环烷基;并且
R5和R6独立地代表氢原子、具有1到6个碳原子的烷基、可被取代的芳烷基或可被取代的芳基;排除以下情况,即R3,R4,R5和R6都代表氢原子,或当R3、R4、R5和R6中的任何一个代表可被取代的甲基时,其他的代表氢原子。
[4]根据上述部分[3]的二胺衍生物,其中R2和R7代表氢原子。
[5]二胺衍生物,其由以下通式(9)表示:
其中,R9代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的杂芳烷基、苯基、4位被取代的苯基或可被取代的杂芳基;
R10和R15独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的芳基或酰基;
R11和R12的中的一个代表甲基,另一个代表氢原子;
R13和R14分别代表氢原子;并且
R16代表苯基、4位被取代的苯基或可被取代的杂芳基。
[6]根据上述部分[5]的二胺衍生物,其中
R9代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、可被取代的芳烷基、可被取代的杂芳烷基、苯基、4位被取代的苯基或可被取代的杂芳基;并且
R10和R15分别代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基、可被取代的芳基或酰基。
[7]根据上述部分[6]的二胺衍生物,其中R10和R15独立地代表氢原子、具有1到6个碳原子的烷基或酰基。
[8]根据上述部分[7]的二胺衍生物,其中R10和R15分别代表氢原子。
[9]杀菌剂,其含有上述部分[1]到[8]中任一项的二胺衍生物作为其活性成分。
[10]上述部分[1]的二胺衍生物的制备方法,其中,具有以下通式(2)的化合物,
其中,R1、R2、R3、R4、R5、R6和R7代表与上述部分[1]中化合物的基团相同的基团,
与具有以下通式(3)的化合物反应,
其中,R8代表与上述部分[1]中的化合物的基团相同的基团,并且,
X代表离去基团。
[11]制备上述部分[1]的二胺衍生物的方法,其中,具有通式(2)的化合物与具有以下通式(4)的化合物进行缩合,
其中,R8代表与上述部分[1]中的化合物的基团相同的基团。
[12]上述部分[1]的二胺衍生物的制备方法,其中,具有以下通式(5)的化合物
其中,R2、R3、R4、R5、R6、R7和R8代表与上述部分[1]中的化合物的基团相同的基团,
与具有以下通式(6)的化合物反应,
其中,R1代表与上述部分[1]中的化合物的基团相同的基团,并且,
X代表离去基团。
[13]上述部分[5]的二胺衍生物的制备方法,其中,具有以下通式(10)的化合物
其中,R9、R10、R11、R12、R13、R14和R15代表与上述部分[5]中的化合物的基团相同的基团,
与具有以下通式(11)的化合物反应,
其中,R16代表与上述部分[5]中的化合物的基团相同的基团,并且
X代表离去基团。
[14]上述部分[5]的二胺衍生物的制备方法,其中,通式(10)的化合物与具有以下通式(12)的化合物进行缩合反应,
其中,R16代表与上述部分[5]中的化合物的基团相同的基团。
[15]上述部分[5]的二胺衍生物的制备方法,其中,具有以下通式(13)的化合物
其中,R10、R11、R12、R13、R14、R15和R16代表与上述部分[5]中的化合物的基团相同的基团,
与具有以下通式(14)的化合物反应,
其中,R9代表与上述部分[5]中的化合物的基团相同的基团,并且,
X代表离去基团。
具体实施方式
下面将对本发明进行更详细的说明。
在通式(1)和(9)的二胺衍生物及其制备方法中,具有1到6个碳原子的烷基的例子包括:甲基、乙基、丙基、丁基、戊基、己基、烯丙基、甲代烯丙基和炔丙基;具有3到6个碳原子的环烷基的例子包括:环丙基、环丁基、环戊基和环己基;具有2到6个碳原子的链烯基的例子包括:乙烯基、丙烯基、丁烯基、戊烯基和己烯基;具有3到6个碳原子的环烯基的例子包括:环丙烯基、环丁烯基、环戊烯基和环己烯基;具有2到6个碳原子的炔基的例子包括:乙炔基、丙炔基、丁炔基、戊炔基和己炔基;芳基的例子包括:苯基和萘基;杂芳基的例子包括:吡啶基,嘧啶基,噻吩基,呋喃基,吡唑基,咪唑基,异噻唑基,异噁唑基,吲哚基,喹啉基,苯并呋喃基,苯并噻吩基,苯并噁唑基,苯并异噁唑基,苯并咪唑基,苯并噻唑基,和苯并异噻唑基;酰基的例子包括:烷基碳酰基例如乙酰基和芳基碳酰基例如苯甲酰基。
芳基和杂芳基的取代基包括具有1到6个碳原子的烷基,例如甲基、乙基、丙基和丁基;具有3到6个碳原子的环烷基,例如环丙基、环丁基、环戊基和环己基;具有1到4个碳原子的卤代烷基,例如三氟甲基、二氟甲基、溴二氟甲基和三氟乙基;具有1到4个碳原子的烷氧基,例如甲氧基、乙氧基、丙氧基和丁氧基;具有1到4个碳原子的卤代烷氧基,例如三氟甲氧基、二氟甲氧基和三氟乙氧基;具有1到4个碳原子的烷硫基,例如甲硫基、乙硫基、丙硫基和丁硫基;具有1到4个碳原子的卤代烷硫基,例如三氟甲硫基、二氟甲硫基和三氟乙硫基;具有1到4个碳原子的烷基亚磺酰基,例如甲基亚磺酰基、乙基亚磺酰基、丙基亚磺酰基和丁基亚磺酰基;具有1到4个碳原子的卤代烷基亚磺酰基,例如三氟甲基亚磺酰基、二氟甲基亚磺酰基和三氟乙基亚磺酰基;具有1到4个碳原子的烷基磺酰基,例如甲基磺酰基、乙基磺酰基、丙基磺酰基和丁基磺酰基;具有1到4个碳原子的卤代烷基磺酰基,例如三氟甲基磺酰基、二氟甲基磺酰基和三氟乙基磺酰基;具有1到4个碳原子的烷基磺酰胺基,例如甲基磺酰胺基、乙基磺酰胺基、丙基磺酰胺基和丁基磺酰胺基;具有1到4个碳原子的卤代烷基磺酰胺基,例如三氟甲基磺酰胺基,二氟甲基磺酰胺基和三氟乙基磺酰胺基;卤原子,例如氟、氯、溴和碘原子;以及酰基,例如乙酰基和苯甲酰基。
芳基和杂芳基可以由它们中选出的两个或两个以上基团取代。
可被取代的甲基的例子包括:甲基,羟甲基和卤代甲基。
在通式(3),(6),(11)和(14)中的化合物中,离去基团的例子包括:卤族原子,例如氯原子;烷氧基,例如甲氧基和乙氧基;芳氧基例如苯氧基;以及咪唑基。
本发明的由通式(1)和(9)表示的化合物具有新颖性。通式(1)的化合物可以由下面反应式(1)表示的过程获得。
反应式(1)
其中,R1、R2、R3、R4、R5、R6和R7分别具有与在通式(2)中相同的定义;并且
R8和X分别与通式(3)中的基团具有相同的定义。
在反应式(1)中,通式(1)的二胺衍生物可以由通式(2)表示的二胺衍生物或其盐与通式(3)表示的已知的羰基化合物反应而得到,反应可以在没有溶剂或有溶剂的情况下进行,也可以在有碱或无碱存在的情况下进行。
在反应式(1)表示的反应中使用的碱的例子包括碱金属氢氧化物,例如氢氧化钠和氢氧化钾;碱土金属氢氧化物,例如氢氧化镁和氢氧化钙;碱金属氢化物,例如氢化钠和氢化钾;碱金属醇化物,例如甲醇钠和乙醇钠;碱金属氧化物,例如氧化钠;碳酸盐,例如碳酸钾和碳酸钠;磷酸盐,例如磷酸三钾,磷酸三钠,磷酸氢二钾和磷酸氢二钠;乙酸盐,例如乙酸钠和乙酸钾;有机碱,例如吡啶,4-(二甲基氨基)吡啶,三乙基胺和1,8-二氮杂双环[5.4.0]十一-7-烯。至少一种碱可用于上述反应中。
对于碱的用量没有特别限定,当至少使用上述有机碱中的一种时,其也可以作为溶剂使用。
反应式(1)表明的反应中使用的溶剂可以包括水;醇,例如甲醇、乙醇、丙醇和丁醇;卤代烃,例如二氯甲烷和氯仿;芳族烃,例如苯,甲苯和二甲苯;脂肪族烃,例如己烷和庚烷;极性非质子溶剂,例如二甲基甲酰胺(DMF),二甲基乙酰胺(DMA),二甲基亚砜(DMSO),1,3-二甲基-2-咪唑啉酮(DMI)和1-甲基-2-吡咯烷酮(NMP);醚,例如二乙醚,二异丙醚,1,2-二甲氧基乙烷(DME),四氢呋喃(THF)和二氧杂环己烷;以及腈,例如乙腈和丙腈。
通式(3)的羰基化合物相对于通式(2)的化合物的化学当量优选为1比2,更优选为1比1.2。
上述反应的反应温度和反应时间可以在较宽范围内变化。通常,反应温度优选在-20到200℃的范围,更优选在0到100℃,反应时间优选在0.01到50小时的范围,更优选为0.1到15小时。
反应式(1)中通式(2)的胺衍生物及其盐,除了市场上可得到的之外,也可以通过如下方式轻易获得,例如:加布里埃耳(Gabriel)合成法;德勒平氏(Delepine)反应;常见的胺合成法,其中氰基,酰胺,亚胺或肟被还原;或者在Tetrahedron Asymmetry,vol.11,1907(2000)中描述的合成法。
反应式(1)中通式(3)的化合物可以按照传统方式制备,其中,通式(4)的已知羧酸衍生物与亚硫酰氯,乙二酰氯,碳酰氯或1,1’-羰基二-1H-咪唑进行反应。
反应式(1)中的通式(3)的化合物也可以按照传统方式制备,其中,通式(4)的已知羧酸衍生物与醇例如甲醇或乙醇在没有催化剂或有催化剂的存在的条件下进行反应。
本发明中通式(1)的化合物也可以由下面反应式(2)表示的过程获得。
反应式(2)
其中,R1、R2、R3、R4、R5、R6和R7分别具有与在通式(2)中相同的定义;并且
R8具有与通式(4)中的基团相同的定义。
在反应式(2)中,通式(1)的二胺衍生物可以通过将通式(2)的二胺衍生物或其盐与通式(4)的已知羧酸衍生物进行缩合反应而得,此反应可以在有溶剂的情况下或在没有溶剂的情况下进行。
这时的缩合剂包括:
N,N’-二环己基碳二亚胺、1,1’-羰基二-1H-咪唑、1-乙基-3-(3-二甲基氨基丙基)碳二亚胺、氯化氢、2-氯-1,3-二甲基咪唑氯(imidazorium chloride)。
对于缩合剂与通式(4)的化合物的用量,前者与后者的化学当量优选为1比2,更优选为1比1.2。
这时的有机溶剂,可以使用与反应式(1)表示的过程中同样的溶剂。
关于通式(4)的羧酸衍生物和通式(2)的化合物的用量,前者与后者的化学当量优选为1比2,更优选为1比1.2。
上述反应的反应温度和反应时间可以在较宽范围变化。通常,反应温度优选在-20到200℃的范围,更优选在0到100℃,反应时间优选在0.01到50小时的范围,更优选为0.1到15小时。
本发明中通式(1)表示的化合物也可以由下面反应式(3)表示的过程获得。
反应式(3)
其中,R2、R3、R4、R5、R6、R7和R8分别与通式(5)中基团具有相同的定义;并且
R1和X分别与通式(6)的基团具有相同的定义。
在反应式(3)中,通式(1)的二胺衍生物可以通过将通式(5)的二胺衍生物或其盐与通式(6)的已知化合物反应而得,反应可以不含溶剂或含有溶剂,也可以在没有碱或在有碱的存在进行。
在该反应中,可以使用与反应式(1)中同样的碱。
对于碱的用量没有特殊限定,当使用上述有机碱时,它们也可以用作溶剂。
此时的溶剂,可以使用在反应式(1)表示的过程中使用的同样的溶剂。
关于通式(6)的化合物与通式(5)的二胺衍生物的用量,前者与后者的化学当量优选为1比2,更优选为1比1.2。
上述反应的反应温度和反应时间可以在较宽范围变化。通常,反应温度优选在-20到200℃的范围,更优选在0到100℃,反应时间优选在0.01到50小时的范围,更优选为0.1到15小时。
通式(9)表示的化合物可以按照同样的方式由上述化合物(10)到(14)取代反应式(1)到(3)中的化合物(2)到(6)得到。
在通式(1)和(9)中的二胺衍生物中存在不对称碳原子,这由取代基的类型所决定,并且衍生物可以以光学异构体,非对映异构体,外消旋变体或其任意比率的混合物的形式存在。本发明包含了这些类型的所有异构体及其混合物。
含有通式(1)和(9)表示的本发明的二胺衍生物作为活性成分的农业和园艺杀菌剂,在控制由稻瘟病菌(Pyricularia oryzae)引起的稻瘟病中显示出优良的效果。
通式(1)和(9)的本发明的二胺衍生物可以将其与至少一种其他杀菌剂、农用化学物质如农药如杀虫剂、除草剂和植物生长调节剂、土壤调节剂和肥料响应物质联合使用。它们可以以混合制剂的形式加以应用。
尽管可以直接应用本发明二胺衍生物,但它们优选作为组合物形式的配方,这可以通过将它们与包括固体或液体稀释液在内的载体进行混合而得到。名词“载体”在这里是指合成的或天然的,无机的或有机的物质,将其混合将有助于活性成分抵达靶点,并且使得活性成分化合物的存储,运输和处理更加容易。
适合在本发明中使用的固体载体的例子包括粘土,例如蒙脱土,高岭石和斑脱土;无机物,例如硅藻土,粘土,滑石,蛭石,石膏,碳酸钙,硅胶和硫酸铵;植物性有机材料,例如大豆粉,锯屑和小麦粉;以及尿素。
适合在本发明中使用的液体载体的例子包括芳族烃,例如甲苯,二甲苯和异丙苯;链烷烃,例如煤油和矿物油;卤代烃,例如四氯化碳,氯仿和二氯乙烷;酮类,例如丙酮和甲基乙酮;醚类,例如二噁烷,四氢呋喃和二甘醇二甲醚;醇类,例如甲醇,乙醇,丙醇和1,2-亚乙基二醇;二甲基甲酰胺;二甲基亚砜;以及水。
为了增强本发明化合物的效力,可以根据目标并考虑到组合物的配方以及应用场所等而单独使用以下助剂中的至少一种,或将它们组合使用。
当致力于化合物的乳化,分散,扩展,湿润,粘结和稳定时,配方中应该使用辅剂。辅剂的例子包括阴离子表面活性剂,例如木质素磺酸盐、烷基苯磺酸盐、烷基硫酸酯、聚氧化烯烷基硫酸酯和聚氧化烯烷基磷酸酯;非离子表面活性剂,例如聚氧化烯烷基醚、聚氧化烯烷基芳基醚、聚氧化烯烷基胺、聚氧化烯烷基酰胺、聚氧化烯烷基硫醚、聚氧化烯脂肪族酯、甘油脂肪酸酯、失水山梨糖醇脂肪酸酯、聚氧化烯失水山梨糖醇脂肪酸酯和聚氧化丙二醇聚氧乙烯嵌段共聚物;润滑剂,例如硬脂酸钙和蜡;稳定剂,例如异丙基氢化二烯磷酸盐(isopropylhydrodienephosphate);甲基纤维素;羧甲基纤维素;酪蛋白;以及阿拉伯树胶。所使用的辅剂并不仅限于上述这些。
作为活性成分的本发明的化合物的一般量分别是:在用于粉末配方时为0.5到20重量%,在用于可乳化浓缩物时为5到50重量%,在用于可湿性粉末时为10到90重量%,在用于颗粒时为0.1到20重量%,在用于易流动物质时为10到90重量%。在每种配方中的载体的一般量分别是:在用于粉末时为60到99重量%,在用于可乳化浓缩物时为40到95重量%,在用于可湿性粉末时为10到90重量%,在用于颗粒时为80到99重量%,在用于易流动物质时为10到90重量%。辅剂的一般量是:在用于粉末时为0.1到20重量%,在用于可乳化浓缩物时为1到20重量%,在用于可湿性粉末时为0.1到20重量%,在用于颗粒时为0.1到20重量%,在用于易流动物质时为0.1到20重量%。
[实施例]
下面以若干实施例及试验例对本发明作进一步详细描述。
实施例1
[N-(甲氧羰基)-N’-苯甲酰基-1-苯基-1,2-乙二胺的制备(化合物No.66)]
将0.22克苯甲酰氯加入到冰水冷却下的10ml的0.25克N-(甲氧羰基)-1-苯基乙二胺和0.2克三乙胺的二氯甲烷溶液中,并将混合物在5℃下搅拌30分钟,以及在室温下搅拌3小时。反应混合物用水清洗,有机层利用无水硫酸镁进行干燥,由减压得到的残余油性物质通过柱色谱在硅胶(2∶1己烷/乙酸乙酯)上进行提纯,获得0.28克的无色结晶的标题化合物。
实施例2
[N-(4-氯苯甲酰)-N’-(异丙氧基羰基)-3-苯基-1,2-丙二胺(化合物No.290)的制备]
将0.21克1,1’-羰基二-1H-咪唑加入到0.19克的4-氯苯甲酸的四氢呋喃溶液中,并在室温下搅拌1小时。然后将5ml的0.25克的2-(异丙氧基羰基氨基)-3-苯基丙胺的四氢呋喃溶液加入上述溶液中,并在室温下搅拌4小时。反应混合物用水清洗,有机层利用无水硫酸镁进行干燥,由减压得到的残余油性物质通过柱色谱在硅胶(2∶1己烷/乙酸乙酯)上进行提纯,获得0.26克的无色结晶的标题化合物。
实施例3
[N-(卞氧基羰基)-N’-苯甲酰基-1-苯基-1,2-乙二胺的制备(化合物No.636)]
将0.12克三乙二胺加入冰水冷却下的10ml的0.25克N-苯甲酰基-2-苯基-1,2-乙二胺盐酸盐和0.17克氯甲酸卞基酯的二氯甲烷溶液中,并将混合物在5℃下搅拌30分钟,以及在室温下搅拌3小时。反应混合物用水清洗,有机层利用无水硫酸镁进行干燥,由减压得到的残余油性物质通过柱色谱在硅胶(2∶1己烷/乙酸乙酯)上进行提纯,获得0.28克的无色结晶的标题化合物。
实施例4
[N-(叔丁氧基羰基)-N’-(4-甲基苯甲酰基)-1-苯基-1,2-乙二胺的制备(化合物No.504)]
将0.24克三乙胺加入到冰水冷却下的0.22克二碳酸二叔丁酯和0.25克N-(4-甲基苯甲酰基)-2-苯基-1,2-乙二胺盐酸盐的二氯甲溶液中,并将混合物在5℃下搅拌1小时,以及在室温下搅拌3小时。反应混合物用水清洗,有机层利用无水硫酸镁进行干燥,由减压得到的残余油性物质通过柱色谱在硅胶(2∶1己烷/乙酸乙酯)上进行提纯,获得0.24克的无色结晶的标题化合物。
可按照与实施例1到4同样的方法得到的通式(1)和(9)的化合物列于如下表1中。这些化合物中的一部分的化合物的物理特性示于表2。表1中的R17到R24是以下通式(15)表示的取代:
表1中,Me代表甲基,Et代表乙基,n-Pr代表正丙基,i-Pr代表异丙基,i-Bu代表异丁基,s-Bu代表仲丁基,t-Bu代表叔丁基,Ph代表苯基,Bn代表卞基,1-Naph代表1-萘基,2-Naph代表2-萘基,c-Pr代表环丙基,c-Hex代表环己基,Ac代表乙酰基,Bz代表苯甲酰基,乙烯基(vinyl)代表乙烯基,烯丙基(allyl)代表2-丙烯基,炔丙基(propargyl)代表2-丙炔基,新戊基(neopentyl)代表2,2-二甲基丙基,甲代烯丙基代表2-甲基-2-丙烯基,以及2-噻吩代表噻吩-2-基。
表1-1
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1 | Me | H | Me | H | H | H | H | Ph |
2 | Me | H | Me | H | H | H | H | 2-ClC6H4 |
3 | Me | H | Me | Me | H | H | H | 3-ClC6H4 |
4 | Me | H | Me | H | H | H | H | 4-ClC6H4 |
5 | Me | H | Me | H | H | H | H | 4-MeC6H4 |
6 | Me | H | Me | H | H | H | H | 4-t-BuC6H4 |
7 | Me | H | Me | H | H | H | H | 1-Naph |
8 | Me | H | Me | H | H | H | H | 噻吩-2-基 |
9 | Me | H | Me | H | H | H | H | 吡啶-3-基 |
10 | Me | H | Me | Me | H | H | H | 4-ClC6H4 |
11 | Me | H | Et | H | H | H | H | Ph |
12 | Me | H | Et | H | H | H | H | 2-ClC6H4 |
13 | Me | H | Et | H | H | H | H | 3-ClC6H4 |
14 | Me | H | Et | H | H | H | H | 4-ClC6H4 |
15 | Me | H | Et | H | H | H | H | 4-MeC6H4 |
16 | Me | H | Et | H | H | H | H | 4-t-BuC6H4 |
17 | Me | H | Et | H | H | H | H | 1-Naph |
18 | Me | H | Et | H | H | H | H | 噻吩-2-基 |
19 | Me | H | Et | H | H | H | H | 2-甲基吡啶-5-基 |
20 | Me | H | Et | Me | H | H | H | 4-ClC6H4 |
21 | Me | H | n-Pr | H | H | H | H | Ph |
22 | Me | H | n-Pr | H | H | H | H | 2-ClC6H4 |
23 | Me | H | n-Pr | H | H | H | H | 4-ClC6H4 |
24 | Me | H | n-Pr | H | H | H | H | 4-MeC6H4 |
25 | Me | H | n-Pr | H | H | H | H | 4-EtC6H4 |
26 | Me | H | i-Pr | H | H | H | H | Ph |
27 | Me | H | i-Pr | H | H | H | H | 4-ClC6H4 |
28 | Me | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
29 | Me | H | i-Pr | H | H | H | H | 2-MeC6H4 |
30 | Me | H | i-Pr | H | H | H | H | 4-MeC6H4 |
31 | Me | H | i-Pr | H | H | H | H | 4-EtC6H4 |
32 | Me | H | i-Pr | H | H | H | H | 2-Naph |
33 | Me | H | i-Pr | H | H | H | H | 5-甲基噻吩-2-基 |
34 | Me | H | i-Pr | H | H | H | H | 吡啶-3-基 |
35 | Me | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
表1-2
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
36 | Me | H | s-Bu | H | H | H | H | Ph |
37 | Me | H | s-Bu | H | H | H | H | 4-ClC6H4 |
38 | Me | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
39 | Me | H | s-Bu | H | H | H | H | 2-MeC6H4 |
40 | Me | H | s-Bu | H | H | H | H | 4-MeC6H4 |
41 | Me | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
42 | Me | H | s-Bu | H | H | H | H | 1-Naph |
43 | Me | H | s-Bu | H | H | H | H | 噻吩-2-基 |
44 | Me | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
45 | Me | H | s-Bu | Me | H | H | H | 4-CF3C6H4 |
46 | Me | H | i-Bu | H | H | H | H | Ph |
47 | Me | H | i-Bu | H | H | H | H | 4-ClC6H4 |
48 | Me | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
49 | Me | H | i-Bu | H | H | H | H | 2-MeC6H4 |
50 | Me | H | i-Bu | H | H | H | H | 4-MeC6H4 |
51 | Me | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
52 | Me | H | i-Bu | H | H | H | H | 2-Naph |
53 | Me | H | i-Bu | H | H | H | H | 噻吩-2-基 |
54 | Me | H | i-Bu | H | H | H | H | 3-甲基异噻唑-5-基 |
55 | Me | H | i-Bu | Me | H | H | H | 4-ClC6H4 |
56 | Me | H | t-Bu | H | H | H | H | Ph |
57 | Me | H | t-Bu | H | H | H | H | 4-ClC6H4 |
58 | Me | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
59 | Me | H | t-Bu | H | H | H | H | 2-MeC6H4 |
60 | Me | H | t-Bu | H | H | H | H | 4-MeC6H4 |
61 | Me | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
62 | Me | H | t-Bu | H | H | H | H | 1-Naph |
63 | Me | H | t-Bu | H | H | H | H | 噻吩-2-基 |
64 | Me | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
65 | Me | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
66 | Me | H | Ph | H | H | H | H | Ph |
67 | Me | H | Ph | H | H | H | H | 2-ClC6H4 |
68 | Me | H | Ph | H | H | H | H | 4-ClC6H4 |
69 | Me | H | Ph | H | H | H | H | 4-MeC6H4 |
70 | Me | H | Ph | H | H | H | H | 4-EtC6H4 |
71 | Me | H | 4-ClC6H4 | H | H | H | H | Ph |
72 | Me | H | 4-ClC6H4 | H | H | H | H | 4-CF3C6H4 |
73 | Me | H | 4-ClC6H4 | H | H | H | H | 2-MeC6H4 |
74 | Me | H | 4-ClC6H4 | H | H | H | H | 4-MeC6H4 |
75 | Me | H | 4-ClC6H4 | H | H | H | H | 4-t-BuC6H4 |
表1-3
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
76 | Me | H | Bn | H | H | H | H | Ph |
77 | Me | H | Bn | H | H | H | H | 4-CF3C6H4 |
78 | Me | H | Bn | H | H | H | H | 2-MeC6H4 |
79 | Me | H | Bn | H | H | H | H | 4-MeC6H4 |
80 | Me | H | Bn | H | H | H | H | 4-EtC6H4 |
81 | Me | H | -(CH2)2- | H | H | H | 4-ClC6H4 | |
82 | Me | H | -(CH2)4- | H | H | H | 4-ClC6H4 | |
83 | Et | H | Me | H | H | H | H | Ph |
84 | Et | H | Me | H | H | H | H | 2-ClC6H4 |
85 | Et | H | Me | H | Me | H | H | 3-ClC6H4 |
86 | Et | H | Me | H | H | H | H | 4-ClC6H4 |
87 | Et | H | Me | H | H | H | H | 4-MeC6H4 |
88 | Et | H | Me | H | H | H | H | 4-t-BuC6H4 |
89 | Et | H | Me | H | H | H | H | 1-Naph |
90 | Et | H | Me | H | H | H | H | 5-氯噻吩-2-基 |
91 | Et | H | Me | H | H | H | H | 吡啶-3-基 |
92 | Et | H | Me | Me | H | H | H | 4-ClC6H4 |
93 | Et | H | Et | H | H | H | H | Ph |
94 | Et | H | Et | H | H | H | H | 2-ClC6H4 |
95 | Et | H | Et | H | H | H | H | 3-ClC6H4 |
96 | Et | H | Et | H | H | H | H | 4-ClC6H4 |
97 | Et | H | Et | H | H | H | H | 4-MeC6H4 |
98 | Et | H | Et | H | H | H | H | 4-t-BuC6H4 |
99 | Et | H | Et | H | H | H | H | 1-Naph |
100 | Et | H | Et | H | H | H | H | 噻吩-2-基 |
101 | Et | H | Et | H | H | H | H | 吡啶-3-基 |
102 | Et | H | Et | Me | H | H | H | 4-ClC6H4 |
103 | Et | H | i-Pr | H | H | H | H | Ph |
104 | Et | H | i-Pr | H | H | H | H | 4-ClC6H4 |
105 | Et | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
106 | Et | H | i-Pr | H | H | H | H | 2-MeC6H4 |
107 | Et | H | i-Pr | H | H | H | H | 4-MeC6H4 |
108 | Et | H | i-Pr | H | H | H | H | 4-EtC6H4 |
109 | Et | H | i-Pr | H | H | H | H | 2-Naph |
110 | Et | H | i-Pr | H | H | H | H | 噻吩-2-基 |
111 | Et | H | i-Pr | H | H | H | H | 4-氯吡啶-3-基 |
112 | Et | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
表1-4
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
113 | Me | H | s-Bu | H | H | H | H | Ph |
114 | Me | H | s-Bu | H | H | H | H | 4-ClC6H4 |
115 | Me | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
116 | Me | H | s-Bu | H | H | H | H | 2-MeC6H4 |
117 | Me | H | s-Bu | H | H | H | H | 4-MeC6H4 |
118 | Me | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
119 | Me | H | s-Bu | H | H | H | H | 1-Naph |
120 | Et | H | s-Bu | H | H | H | H | 噻吩-2-基 |
121 | Et | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
122 | Et | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
123 | Et | H | i-Bu | H | H | H | H | Ph |
124 | Et | H | i-Bu | H | H | H | H | 4-ClC6H4 |
125 | Et | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
126 | Et | H | i-Bu | H | H | H | H | 2-MeC6H4 |
127 | Et | H | i-Bu | H | H | H | H | 4-MeC6H4 |
128 | Et | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
129 | Et | H | i-Bu | H | H | H | H | 1-Naph |
130 | Et | H | i-Bu | H | H | H | H | 噻吩-2-基 |
131 | Et | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
132 | Et | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
133 | Et | H | t-Bu | H | H | H | H | Ph |
134 | Et | H | t-Bu | H | H | H | H | 4-ClC6H4 |
135 | Et | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
136 | Et | H | t-Bu | H | H | H | H | 2-MeC6H4 |
137 | Et | H | t-Bu | H | H | H | H | 4-MeC6H4 |
138 | Et | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
139 | Et | H | t-Bu | H | H | H | H | 1-Naph |
140 | Et | H | t-Bu | H | H | H | H | 噻吩-2-基 |
141 | Et | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
142 | Et | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
143 | Et | H | Ph | H | H | H | H | Ph |
144 | Et | H | Ph | H | H | H | H | 2-ClC6H4 |
145 | Et | H | Ph | H | H | H | H | 4-ClC6H4 |
146 | Et | H | Ph | H | H | H | H | 4-MeC6H4 |
147 | Et | H | Ph | H | H | H | H | 4-EtC6H4 |
表1-5
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
148 | n-Pr | H | Me | H | H | H | H | Ph |
149 | n-Pr | H | Me | H | H | H | H | 2-ClC6H4 |
150 | n-Pr | H | Me | Me | H | H | H | 3-ClC6H4 |
151 | n-Pr | H | Me | H | H | H | H | 4-ClC6H4 |
152 | n-Pr | H | Me | H | H | H | H | 4-MeC6H4 |
153 | n-Pr | H | Me | H | H | H | H | 4-t-BuC6H4 |
154 | n-Pr | H | Me | H | H | H | H | 1-Naph |
155 | n-Pr | H | Me | H | H | H | H | 5-乙基噻吩-2-基 |
156 | n-Pr | H | Me | H | H | H | H | 吡啶-3-基 |
157 | n-Pr | H | Me | Me | H | H | H | 4-ClC6H4 |
158 | n-Pr | H | Et | H | Et | H | H | Ph |
159 | n-Pr | H | Et | H | Et | H | H | 2-ClC6H4 |
160 | n-Pr | H | Et | H | Et | H | H | 3-ClC6H4 |
161 | n-Pr | H | Et | H | Et | H | H | 4-ClC6H4 |
162 | n-Pr | H | Et | H | Et | H | H | 4-MeC6H4 |
163 | n-Pr | H | Et | H | Et | H | H | 4-t-BuC6H4 |
164 | n-Pr | H | Et | H | Et | H | H | 1-Naph |
165 | n-Pr | H | Et | H | Et | H | H | 噻吩-2-基 |
166 | n-Pr | H | Et | H | Et | H | H | 吡啶-3-基 |
167 | n-Pr | H | Et | Me | Et | H | H | 4-ClC6H4 |
168 | n-Pr | H | i-Pr | H | H | H | H | Ph |
168 | n-Pr | H | i-Pr | H | H | H | H | 4-ClC6H4 |
169 | n-Pr | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
170 | n-Pr | H | i-Pr | H | H | H | H | 2-MeC6H4 |
171 | n-Pr | H | i-Pr | H | H | H | H | 4-MeC6H4 |
172 | n-Pr | H | i-Pr | H | H | H | H | 4-EtC6H4 |
173 | n-Pr | H | i-Pr | H | H | H | H | 2-Naph |
174 | n-Pr | H | i-Pr | H | H | H | H | 噻吩-2-基 |
175 | n-Pr | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
176 | n-Pr | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
177 | n-Pr | H | s-Bu | H | Me | Me | H | Ph |
178 | n-Pr | H | s-Bu | H | Me | Me | H | 4-ClC6H4 |
179 | n-Pr | H | s-Bu | H | Me | Me | H | 3,4-Cl2C6H3 |
180 | n-Pr | H | s-Bu | H | Me | Me | H | 2-MeC6H4 |
181 | n-Pr | H | s-Bu | H | Me | Me | H | 4-MeC6H4 |
182 | n-Pr | H | s-Bu | H | Me | Me | H | 4-t-BuC6H4 |
183 | n-Pr | H | s-Bu | H | Me | Me | H | 1-Naph |
184 | n-Pr | H | s-Bu | H | Me | Me | H | 噻吩-2-基 |
185 | n-Pr | H | s-Bu | H | Me | Me | H | 异噻唑-5-基 |
186 | n-Pr | H | s-Bu | Me | Me | Me | H | 4-MeC6H4 |
表1-6
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
187 | n-Pr | H | i-Bu | H | H | H | H | 4-ClC6H4 |
188 | n-Pr | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
189 | n-Pr | H | i-Bu | H | H | H | H | 2-MeC6H4 |
190 | n-Pr | H | i-Bu | H | H | H | H | 4-MeC6H4 |
191 | n-Pr | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
192 | n-Pr | H | i-Bu | H | H | H | H | 1-Naph |
193 | n-Pr | H | i-Bu | H | H | H | H | 噻吩-2-基 |
194 | n-Pr | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
195 | n-Pr | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
196 | n-Pr | H | t-Bu | H | H | H | H | Ph |
197 | n-Pr | H | t-Bu | H | H | H | H | 4-ClC6H4 |
198 | n-Pr | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
199 | n-Pr | H | t-Bu | H | H | H | H | 2-MeC6H4 |
200 | n-Pr | H | t-Bu | H | H | H | H | 4-MeC6H4 |
201 | n-Pr | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
202 | n-Pr | H | t-Bu | H | H | H | H | 1-Naph |
203 | n-Pr | H | t-Bu | H | H | H | H | 噻吩-2-基 |
204 | n-Pr | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
205 | n-Pr | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
206 | n-Pr | H | Ph | H | H | H | H | Ph |
207 | n-Pr | H | Ph | H | H | H | H | 2-ClC6H4 |
208 | n-Pr | H | Ph | H | H | H | H | 4-ClC6H4 |
209 | n-Pr | H | Ph | H | H | H | H | 4-MeC6H4 |
210 | n-Pr | H | Ph | H | H | H | H | 4-EtC6H4 |
211 | i-Pr | H | Me | H | H | H | H | Ph |
212 | i-Pr | H | Me | H | H | H | H | 2-ClC6H4 |
213 | i-Pr | H | Me | H | Me | H | H | 3-ClC6H4 |
214 | i-Pr | H | Me | H | H | H | H | 4-ClC6H4 |
215 | i-Pr | H | Me | H | H | H | H | 4-MeC6H4 |
216 | i-Pr | H | Me | H | H | H | H | 4-t-BuC6H4 |
217 | i-Pr | H | Me | H | H | H | H | 1-Naph |
218 | i-Pr | H | Me | H | H | H | H | 噻吩-2-基 |
219 | i-Pr | H | Me | H | H | H | H | 吡啶-3-基 |
220 | i-Pr | H | Me | Me | H | H | H | 4-ClC6H4 |
表1-7
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
221 | i-Pr | H | Et | H | H | H | H | Ph |
222 | i-Pr | H | Et | H | H | H | H | 2-ClC6H4 |
223 | i-Pr | H | Et | H | H | H | H | 3-ClC6H4 |
224 | i-Pr | H | Et | H | H | H | H | 4-ClC6H4 |
225 | i-Pr | H | Et | H | H | H | H | 4-MeC6H4 |
226 | i-Pr | H | Et | H | H | H | H | 4-t-BuC6H4 |
227 | i-Pr | H | Et | H | H | H | H | 1-Naph |
228 | i-Pr | H | Et | H | H | H | H | 噻吩-2-基 |
229 | i-Pr | H | Et | H | H | H | H | 2-甲基吡啶-5-基 |
230 | i-Pr | H | Et | Me | H | H | H | 4-ClC6H4 |
231 | i-Pr | H | n-Pr | H | H | H | H | Ph |
232 | i-Pr | H | n-Pr | H | H | H | H | 2-ClC6H4 |
233 | i-Pr | H | n-Pr | H | H | H | H | 4-ClC6H4 |
234 | i-Pr | H | n-Pr | H | H | H | H | 4-MeC6H4 |
235 | i-Pr | H | n-Pr | H | H | H | H | 4-EtC6H4 |
236 | i-Pr | H | i-Pr | H | H | H | H | Ph |
237 | i-Pr | H | i-Pr | H | H | H | H | 4-ClC6H4 |
238 | i-Pr | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
239 | i-Pr | H | i-Pr | H | H | H | H | 2-MeC6H4 |
240 | i-Pr | H | i-Pr | H | H | H | H | 4-MeC6H4 |
241 | i-Pr | H | i-Pr | H | H | H | H | 4-EtC6H4 |
242 | i-Pr | H | i-Pr | H | H | H | H | 2-Naph |
243 | i-Pr | H | i-Pr | H | H | H | H | 5-甲基噻吩-2-基 |
244 | i-Pr | H | i-Pr | H | H | H | H | 吡啶-3-基 |
245 | i-Pr | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
246 | i-Pr | H | i-Pr | H | Me | H | H | 4-MeC6H4 |
247 | i-Pr | H | i-Pr | H | Me | H | H | 4-ClC6H4 |
248 | i-Pr | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
249 | i-Pr | H | s-Bu | H | H | H | H | 2-MeC6H4 |
250 | i-Pr | H | s-Bu | H | H | H | H | 4-MeC6H4 |
251 | i-Pr | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
252 | i-Pr | H | s-Bu | H | H | H | H | 1-Naph |
253 | i-Pr | H | s-Bu | H | H | H | H | 噻吩-2-基 |
254 | i-Pr | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
255 | i-Pr | H | s-Bu | Me | H | H | H | 4-CF3C6H4 |
表1-8
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
256 | i-Pr | H | i-Bu | H | H | H | H | Ph |
257 | i-Pr | H | i-Bu | H | H | H | H | 4-ClC6H4 |
258 | i-Pr | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
259 | i-Pr | H | i-Bu | H | H | H | H | 2-MeC6H4 |
260 | i-Pr | H | i-Bu | H | H | H | H | 4-MeC6H4 |
261 | i-Pr | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
262 | i-Pr | H | i-Bu | H | H | H | H | 2-Naph |
263 | i-Pr | H | i-Bu | H | H | H | H | 噻吩-2-基 |
264 | i-Pr | H | i-Bu | H | H | H | H | 3-甲基异噻唑-5-基 |
265 | i-Pr | H | i-Bu | Me | H | H | H | 4-ClC6H4 |
266 | i-Pr | H | t-Bu | H | H | H | H | Ph |
267 | i-Pr | H | t-Bu | H | H | H | H | 4-ClC6H4 |
268 | i-Pr | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
269 | i-Pr | H | t-Bu | H | H | H | H | 2-MeC6H4 |
270 | i-Pr | H | t-Bu | H | H | H | H | 4-MeC6H4 |
271 | i-Pr | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
272 | i-Pr | H | t-Bu | H | H | H | H | 1-Naph |
273 | i-Pr | H | t-Bu | H | H | H | H | 噻吩-2-基 |
274 | i-Pr | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
275 | i-Pr | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
276 | i-Pr | H | Ph | H | H | H | H | Ph |
277 | i-Pr | H | Ph | H | H | H | H | 2-ClC6H4 |
278 | i-Pr | H | Ph | H | H | H | H | 4-ClC6H4 |
279 | i-Pr | H | Ph | H | H | H | H | 4-MeC6H4 |
280 | i-Pr | H | Ph | H | H | H | H | 4-EtC6H4 |
281 | i-Pr | H | 4-ClC6H4 | H | H | H | H | Ph |
282 | i-Pr | H | 4-ClC6H4 | H | H | H | H | 4-CF3C6H4 |
283 | i-Pr | H | 4-ClC6H4 | H | H | H | H | 2-MeC6H4 |
284 | i-Pr | H | 4-ClC6H4 | H | H | H | H | 4-MeC6H4 |
285 | i-Pr | H | 4-ClC6H4 | H | H | H | H | 4-t-BuC6H4 |
286 | i-Pr | H | Bn | H | H | H | H | Ph |
287 | i-Pr | H | Bn | H | H | H | H | 4-CF3C6H4 |
288 | i-Pr | H | Bn | H | H | H | H | 2-MeC6H4 |
289 | i-Pr | H | Bn | H | H | H | H | 4-MeC6H4 |
290 | i-Pr | H | Bn | H | H | H | H | 4-ClC6H4 |
291 | i-Pr | H | -(CH2)4- | H | H | H | 4-ClC6H4 | |
292 | i-Pr | H | -(CH2)5- | H | H | H | 4-ClC6H4 |
表1-9
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
293 | s-Bu | H | Me | H | H | H | H | Ph |
294 | s-Bu | H | Me | H | H | H | H | 2-ClC6H4 |
295 | s-Bu | H | Me | H | Me | H | H | 3-ClC6H4 |
296 | s-Bu | H | Me | H | H | H | H | 4-ClC6H4 |
297 | s-Bu | H | Me | H | H | H | H | 4-MeC6H4 |
298 | s-Bu | H | Me | H | H | H | H | 4-t-BuC6H4 |
299 | s-Bu | H | Me | H | H | H | H | 1-Naph |
300 | s-Bu | H | Me | H | H | H | H | 3-甲基噻吩-2-基 |
301 | s-Bu | H | Me | H | H | H | H | 吡啶-3-基 |
302 | s-Bu | H | Me | Me | H | H | H | 4-ClC6H4 |
303 | s-Bu | Ac | Et | H | H | H | H | Ph |
304 | s-Bu | Ac | Et | H | H | H | H | 2-ClC6H4 |
305 | s-Bu | Ac | Et | H | H | H | H | 3-ClC6H4 |
306 | s-Bu | Ac | Et | H | H | H | H | 4-ClC6H4 |
307 | s-Bu | Ac | Et | H | H | H | H | 4-MeC6H4 |
308 | s-Bu | Ac | Et | H | H | H | H | 4-t-BuC6H4 |
309 | s-Bu | Ac | Et | H | H | H | H | 1-Naph |
310 | s-Bu | Ac | Et | H | H | H | H | 噻吩-2-基 |
311 | s-Bu | Ac | Et | H | H | H | H | 吡啶-3-基 |
312 | s-Bu | Ac | Et | Me | H | H | H | 4-ClC6H4 |
313 | s-Bu | H | i-Pr | H | H | H | H | Ph |
314 | s-Bu | H | i-Pr | H | H | H | H | 4-ClC6H4 |
315 | s-Bu | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
316 | s-Bu | H | i-Pr | H | H | H | H | 2-MeC6H4 |
317 | s-Bu | H | i-Pr | H | H | H | H | 4-MeC6H4 |
318 | s-Bu | H | i-Pr | H | H | H | H | 4-EtC6H4 |
319 | s-Bu | H | i-Pr | H | H | H | H | 2-Naph |
320 | s-Bu | H | i-Pr | H | H | H | H | 噻吩-2-基 |
321 | s-Bu | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
322 | s-Bu | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
323 | s-Bu | H | s-Bu | H | H | H | Bz | Ph |
324 | s-Bu | H | s-Bu | H | H | H | Bz | 4-ClC6H4 |
325 | s-Bu | H | s-Bu | H | H | H | Bz | 3,4-Cl2C6H3 |
326 | s-Bu | H | s-Bu | H | H | H | Bz | 2-MeC6H4 |
327 | s-Bu | H | s-Bu | H | H | H | Bz | 4-MeC6H4 |
328 | s-Bu | H | s-Bu | H | H | H | Bz | 4-t-BuC6H4 |
329 | s-Bu | H | s-Bu | H | H | H | Bz | 1-Naph |
330 | s-Bu | H | s-Bu | H | H | H | Bz | 噻吩-2-基 |
331 | s-Bu | H | s-Bu | H | H | H | Bz | 异噻唑-5-基 |
332 | s-Bu | H | s-Bu | Me | H | H | Bz | 4-MeC6H4 |
表1-10
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
333 | s-Bu | H | i-Bu | H | H | H | H | Ph |
334 | s-Bu | H | i-Bu | H | H | H | H | 4-ClC6H4 |
335 | s-Bu | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
336 | s-Bu | H | i-Bu | H | H | H | H | 2-MeC6H4 |
337 | s-Bu | H | i-Bu | H | H | H | H | 4-MeC6H4 |
338 | s-Bu | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
339 | s-Bu | H | i-Bu | H | H | H | H | 1-Naph |
340 | s-Bu | H | i-Bu | H | H | H | H | 噻吩-2-基 |
341 | s-Bu | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
342 | s-Bu | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
343 | s-Bu | Ac | t-Bu | H | H | H | H | Ph |
344 | s-Bu | Ac | t-Bu | H | H | H | H | 4-ClC6H4 |
345 | s-Bu | Ac | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
346 | s-Bu | Ac | t-Bu | H | H | H | H | 2-MeC6H4 |
347 | s-Bu | Ac | t-Bu | H | H | H | H | 4-MeC6H4 |
348 | s-Bu | Ac | t-Bu | H | H | H | H | 4-t-BuC6H4 |
349 | s-Bu | Ac | t-Bu | H | H | H | H | 1-Naph |
350 | s-Bu | Ac | t-Bu | H | H | H | H | 噻吩-2-基 |
351 | s-Bu | Ac | t-Bu | H | H | H | H | 异噻唑-5-基 |
352 | s-Bu | Ac | t-Bu | Me | H | H | H | 4-MeC6H4 |
353 | s-Bu | H | Ph | H | H | H | H | Ph |
354 | s-Bu | H | Ph | H | H | H | H | 2-ClC6H4 |
355 | s-Bu | H | Ph | H | H | H | H | 4-ClC6H4 |
356 | s-Bu | H | Ph | H | H | H | H | 4-MeC6H4 |
357 | s-Bu | H | Ph | H | H | H | H | 4-EtC6H4 |
358 | i-Bu | H | Me | H | H | H | H | Ph |
359 | i-Bu | H | Me | H | H | H | H | 2-ClC6H4 |
360 | i-Bu | H | Me | Me | H | H | H | 3-ClC6H4 |
361 | i-Bu | H | Me | H | H | H | H | 4-ClC6H4 |
362 | i-Bu | H | Me | H | H | H | H | 4-MeC6H4 |
363 | i-Bu | H | Me | H | H | H | H | 4-t-BuC6H4 |
364 | i-Bu | H | Me | H | H | H | H | 1-Naph |
365 | i-Bu | H | Me | H | H | H | H | 噻吩-2-基 |
366 | i-Bu | H | Me | H | H | H | H | 吡啶-3-基 |
367 | i-Bu | H | Me | Me | H | H | H | 4-ClC6H4 |
表1-11
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
368 | i-Bu | H | Et | H | H | H | H | Ph |
369 | i-Bu | H | Et | H | H | H | H | 2-ClC6H4 |
370 | i-Bu | H | Et | H | H | H | H | 3-ClC6H4 |
371 | i-Bu | H | Et | H | H | H | H | 4-ClC6H4 |
372 | i-Bu | H | Et | H | H | H | H | 4-MeC6H4 |
373 | i-Bu | H | Et | H | H | H | H | 4-t-BuC6H4 |
374 | i-Bu | H | Et | H | H | H | H | 1-Naph |
375 | i-Bu | H | Et | H | H | H | H | 噻吩-2-基 |
376 | i-Bu | H | Et | H | H | H | H | 2-甲基吡啶-5-基 |
377 | i-Bu | H | Et | Me | H | H | H | 4-ClC6H4 |
378 | i-Bu | H | n-Pr | H | H | H | H | Ph |
379 | i-Bu | H | n-Pr | H | H | H | H | 2-ClC6H4 |
380 | i-Bu | H | n-Pr | H | H | H | H | 4-ClC6H4 |
381 | i-Bu | H | n-Pr | H | H | H | H | 4-MeC6H4 |
382 | i-Bu | H | n-Pr | H | H | H | H | 4-EtC6H4 |
383 | i-Bu | H | i-Pr | H | H | H | H | Ph |
384 | i-Bu | H | i-Pr | H | H | H | H | 4-ClC6H4 |
385 | i-Bu | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
386 | i-Bu | H | i-Pr | H | H | H | H | 2-MeC6H4 |
387 | i-Bu | H | i-Pr | H | H | H | H | 4-MeC6H4 |
388 | i-Bu | H | i-Pr | H | H | H | H | 4-EtC6H4 |
389 | i-Bu | H | i-Pr | H | H | H | H | 2-Naph |
390 | i-Bu | H | i-Pr | H | H | H | H | 5-甲基噻吩-2-基 |
391 | i-Bu | H | i-Pr | H | H | H | H | 吡啶-3-基 |
392 | i-Bu | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
393 | i-Bu | H | s-Bu | H | H | H | H | Ph |
394 | i-Bu | H | s-Bu | H | H | H | H | 4-ClC6H4 |
395 | i-Bu | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
396 | i-Bu | H | s-Bu | H | H | H | H | 2-MeC6H4 |
397 | i-Bu | H | s-Bu | H | H | H | H | 4-MeC6H4 |
398 | i-Bu | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
399 | i-Bu | H | s-Bu | H | H | H | H | 1-Naph |
400 | i-Bu | H | s-Bu | H | H | H | H | 噻吩-2-基 |
401 | i-Bu | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
402 | i-Bu | H | s-Bu | Me | H | H | H | 4-CF3C6H4 |
表1-12
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
403 | i-Bu | H | i-Bu | H | H | H | H | Ph |
404 | i-Bu | H | i-Bu | H | H | H | H | 4-ClC6H4 |
405 | i-Bu | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
406 | i-Bu | H | i-Bu | H | H | H | H | 2-MeC6H4 |
407 | i-Bu | H | i-Bu | H | H | H | H | 4-MeC6H4 |
408 | i-Bu | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
409 | i-Bu | H | i-Bu | H | H | H | H | 2-Naph |
410 | i-Bu | H | i-Bu | H | H | H | H | 噻吩-2-基 |
411 | i-Bu | H | i-Bu | H | H | H | H | 3-甲基异噻唑-5-基 |
412 | i-Bu | H | i-Bu | Me | H | H | H | 4-ClC6H4 |
413 | i-Bu | Ac | t-Bu | H | H | H | H | Ph |
414 | i-Bu | Ac | t-Bu | H | H | H | H | 4-ClC6H4 |
415 | i-Bu | Ac | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
416 | i-Bu | Ac | t-Bu | H | H | H | H | 2-MeC6H4 |
417 | i-Bu | Ac | t-Bu | H | H | H | H | 4-MeC6H4 |
418 | i-Bu | Ac | t-Bu | H | H | H | H | 4-t-BuC6H4 |
419 | i-Bu | Ac | t-Bu | H | H | H | H | 1-Naph |
420 | i-Bu | Ac | t-Bu | H | H | H | H | 噻吩-2-基 |
421 | i-Bu | Ac | t-Bu | H | H | H | H | 异噻唑-5-基 |
422 | i-Bu | Ac | t-Bu | Me | H | H | H | 4-MeC6H4 |
423 | i-Bu | H | Ph | H | H | H | H | Ph |
424 | i-Bu | H | Ph | H | H | H | H | 2-ClC6H4 |
425 | i-Bu | H | Ph | H | H | H | H | 4-ClC6H4 |
426 | i-Bu | H | Ph | H | H | H | H | 4-MeC6H4 |
427 | i-Bu | H | Ph | H | H | H | H | 4-EtC6H4 |
428 | i-Bu | H | 4-ClC6H4 | H | H | H | H | Ph |
429 | i-Bu | H | 4-ClC6H4 | H | H | H | H | 4-CF3C6H4 |
430 | i-Bu | H | 4-ClC6H4 | H | H | H | H | 2-MeC6H4 |
431 | i-Bu | H | 4-ClC6H4 | H | H | H | H | 4-MeC6H4 |
432 | i-Bu | H | 4-ClC6H4 | H | H | H | H | 4-t-BuC6H4 |
433 | i-Bu | H | Bn | H | H | H | Bz | Ph |
434 | i-Bu | H | Bn | H | H | H | Bz | 4-CF3C6H4 |
435 | i-Bu | H | Bn | H | H | H | Bz | 2-MeC6H4 |
436 | i-Bu | H | Bn | H | H | H | Bz | 4-MeC6H4 |
437 | i-Bu | H | Bn | H | H | H | Bz | 4-EtC6H4 |
438 | i-Bu | H | -(CH2)4- | H | H | Bz | 4-ClC6H4 | |
439 | i-Bu | H | -(CH2)5- | H | H | Bz | 4-ClC6H4 |
表1-13
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
440 | t-Bu | H | Me | H | H | H | H | Ph |
441 | t-Bu | H | Me | H | H | H | H | 2-ClC6H4 |
442 | t-Bu | H | Me | H | Et | H | H | 3-ClC6H4 |
443 | t-Bu | H | Me | H | H | H | H | 4-ClC6H4 |
444 | t-Bu | H | Me | H | H | H | H | 4-MeC6H4 |
445 | t-Bu | H | Me | H | H | H | H | 4-t-BuC6H4 |
446 | t-Bu | H | Me | H | H | H | H | 1-Naph |
447 | t-Bu | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
448 | t-Bu | H | Me | H | H | H | H | 吡啶-3-基 |
449 | t-Bu | H | Me | Me | H | H | H | 4-ClC6H4 |
450 | t-Bu | Me | Et | H | H | H | H | Ph |
451 | t-Bu | Me | Et | H | H | H | H | 2-ClC6H4 |
452 | t-Bu | Me | Et | H | H | H | H | 3-ClC6H4 |
453 | t-Bu | Me | Et | H | H | H | H | 4-ClC6H4 |
454 | t-Bu | Me | Et | H | H | H | H | 4-MeC6H4 |
455 | t-Bu | Me | Et | H | H | H | H | 4-t-BuC6H4 |
456 | t-Bu | Me | Et | H | H | H | H | 1-Naph |
457 | t-Bu | Me | Et | H | H | H | H | 噻吩-2-基 |
458 | t-Bu | Me | Et | H | H | H | H | 吡啶-3-基 |
459 | t-Bu | Me | Et | Me | H | H | H | 4-ClC6H4 |
460 | t-Bu | H | i-Pr | H | H | H | H | Ph |
461 | t-Bu | H | i-Pr | H | H | H | H | 4-ClC6H4 |
462 | t-Bu | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
463 | t-Bu | H | i-Pr | H | H | H | H | 2-MeC6H4 |
464 | t-Bu | H | i-Pr | H | H | H | H | 4-MeC6H4 |
465 | t-Bu | H | i-Pr | H | H | H | H | 4-EtC6H4 |
466 | t-Bu | H | i-Pr | H | H | H | H | 2-Naph |
467 | t-Bu | H | i-Pr | H | H | H | H | 噻吩-2-基 |
468 | t-Bu | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
469 | t-Bu | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
470 | t-Bu | H | i-Pr | H | Me | H | Et | 4-MeC6H4 |
471 | t-Bu | H | i-Pr | H | Me | H | Et | 4-ClC6H4 |
472 | t-Bu | H | s-Bu | H | H | H | Et | 3,4-Cl2C6H3 |
473 | t-Bu | H | s-Bu | H | H | H | Et | 2-MeC6H4 |
474 | t-Bu | H | s-Bu | H | H | H | Et | 4-MeC6H4 |
475 | t-Bu | H | s-Bu | H | H | H | Et | 4-t-BuC6H4 |
476 | t-Bu | H | s-Bu | H | H | H | Et | 1-Naph |
478 | t-Bu | H | s-Bu | H | H | H | Et | 噻吩-2-基 |
479 | t-Bu | H | s-Bu | H | H | H | Et | 异噻唑-5-基 |
480 | t-Bu | H | s-Bu | Me | H | H | Et | 4-MeC6H4 |
表1-14
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
481 | t-Bu | H | i-Bu | H | H | H | H | Ph |
482 | t-Bu | H | i-Bu | H | H | H | H | 4-ClC6H4 |
483 | t-Bu | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
484 | t-Bu | H | i-Bu | H | H | H | H | 2-MeC6H4 |
485 | t-Bu | H | i-Bu | H | H | H | H | 4-MeC6H4 |
486 | t-Bu | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
487 | t-Bu | H | i-Bu | H | H | H | H | 1-Naph |
488 | t-Bu | H | i-Bu | H | H | H | H | 噻吩-2-基 |
489 | t-Bu | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
490 | t-Bu | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
491 | t-Bu | H | t-Bu | H | H | H | H | Ph |
492 | t-Bu | H | t-Bu | H | H | H | H | 4-ClC6H4 |
493 | t-Bu | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
494 | t-Bu | H | t-Bu | H | H | H | H | 2-MeC6H4 |
495 | t-Bu | H | t-Bu | H | H | H | H | 4-MeC6H4 |
496 | t-Bu | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
497 | t-Bu | H | t-Bu | H | H | H | H | 1-Naph |
498 | t-Bu | H | t-Bu | H | H | H | H | 噻吩-2-基 |
499 | t-Bu | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
500 | t-Bu | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
501 | t-Bu | H | Ph | H | H | H | H | Ph |
502 | t-Bu | H | Ph | H | H | H | H | 2-ClC6H4 |
503 | t-Bu | H | Ph | H | H | H | H | 4-ClC6H4 |
504 | t-Bu | H | Ph | H | H | H | H | 4-MeC6H4 |
505 | t-Bu | H | Ph | H | H | H | H | 4-EtC6H4 |
506 | Ph | H | Me | H | H | H | H | Ph |
507 | Ph | H | Me | H | H | H | H | 2-ClC6H4 |
508 | Ph | H | Me | Me | H | H | H | 3-ClC6H4 |
509 | Ph | H | Me | H | H | H | H | 4-ClC6H4 |
510 | Ph | H | Me | H | H | H | H | 4-MeC6H4 |
511 | Ph | H | Me | H | H | H | H | 4-t-BuC6H4 |
512 | Ph | H | Me | H | H | H | H | 1-Naph |
513 | Ph | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
514 | Ph | H | Me | H | H | H | H | 吡啶-3-基 |
515 | Ph | H | Me | Me | H | H | H | 4-ClC6H4 |
表1-15
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
516 | Ph | H | Et | H | H | H | H | Ph |
517 | ph | H | Et | H | H | H | H | 2-ClC6H4 |
518 | Ph | H | Et | H | H | H | H | 3-ClC6H4 |
519 | Ph | H | Et | H | H | H | H | 4-ClC6H4 |
520 | Ph | H | Et | H | H | H | H | 4-MeC6H4 |
521 | Ph | H | Et | H | H | H | H | 4-t-BuC6H4 |
522 | Ph | H | Et | H | H | H | H | 1-Naph |
523 | Ph | H | Et | H | H | H | H | 噻吩-2-基 |
524 | Ph | H | Et | H | H | H | H | 吡啶-3-基 |
525 | Ph | H | Et | Me | H | H | H | 4-ClC6H4 |
526 | Ph | H | i-Pr | H | H | H | H | Ph |
527 | Ph | H | i-Pr | H | H | H | H | 4-ClC6H4 |
528 | Ph | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
529 | Ph | H | i-Pr | H | H | H | H | 2-MeC6H4 |
530 | Ph | H | i-Pr | H | H | H | H | 4-MeC6H4 |
531 | Ph | H | i-Pr | H | H | H | H | 4-EtC6H4 |
532 | Ph | H | i-Pr | H | H | H | H | 2-Naph |
533 | Ph | H | i-Pr | H | H | H | H | 噻吩-2-基 |
534 | Ph | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
535 | Ph | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
536 | Ph | H | 烯丙基 | H | H | H | H | Ph |
537 | Ph | H | 烯丙基 | H | H | H | H | 4-ClC6H4 |
538 | Ph | H | 烯丙基 | H | H | H | H | 3,4-Cl2C6H3 |
539 | Ph | H | 烯丙基 | H | H | H | H | 2-MeC6H4 |
540 | Ph | H | 烯丙基 | H | H | H | H | 4-MeC6H4 |
541 | Ph | H | 烯丙基 | H | H | H | H | 4-t-BuC6H4 |
542 | Ph | H | 烯丙基 | H | H | H | H | 1-Naph |
543 | Ph | H | 烯丙基 | H | H | H | H | 噻吩-2-基 |
544 | Ph | H | 烯丙基 | H | H | H | H | 异噻唑-5-基 |
545 | Ph | H | 烯丙基 | Me | H | H | H | 4-MeC6H4 |
546 | Ph | H | i-Bu | H | H | H | H | Ph |
547 | Ph | H | i-Bu | H | H | H | H | 4-ClC6H4 |
548 | Ph | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
549 | Ph | H | i-Bu | H | H | H | H | 2-MeC6H4 |
550 | Ph | H | i-Bu | H | H | H | H | 4-MeC6H4 |
551 | Ph | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
552 | Ph | H | i-Bu | H | H | H | H | 1-Naph |
553 | Ph | H | i-Bu | H | H | H | H | 噻吩-2-基 |
554 | Ph | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
555 | Ph | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
表1-16
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
556 | Ph | H | 炔丙基 | H | H | H | H | Ph |
557 | Ph | H | 炔丙基 | H | H | H | H | 4-ClC6H4 |
558 | Ph | H | 炔丙基 | H | H | H | H | 3,4-Cl2C6H3 |
559 | Ph | H | 炔丙基 | H | H | H | H | 2-MeC6H4 |
560 | Ph | H | 炔丙基 | H | H | H | H | 4-MeC6H4 |
561 | Ph | H | 炔丙基 | H | H | H | H | 4-t-BuC6H4 |
562 | Ph | H | 炔丙基 | H | H | H | H | 1-Naph |
563 | Ph | H | 炔丙基 | H | H | H | H | 噻吩-2-基 |
564 | Ph | H | 炔丙基 | H | H | H | H | 异噻唑-5-基 |
565 | Ph | H | 炔丙基 | Me | H | H | H | 4-MeC6H4 |
566 | Ph | H | Ph | H | H | H | H | Ph |
567 | Ph | H | Ph | H | H | H | H | 2-ClC6H4 |
568 | Ph | H | Ph | H | H | H | H | 4-ClC6H4 |
569 | Ph | H | Ph | H | H | H | H | 4-MeC6H4 |
570 | Ph | H | Ph | H | H | H | H | 4-EtC6H4 |
571 | Bn | H | Me | H | H | H | H | Ph |
572 | Bn | H | Me | H | H | H | H | 2-ClC6H4 |
573 | Bn | H | Me | H | Me | H | H | 3-ClC6H4 |
574 | Bn | H | Me | H | H | H | H | 4-ClC6H4 |
575 | Bn | H | Me | H | H | H | H | 4-MeC6H4 |
576 | Bn | H | Me | H | H | H | H | 4-t-BuC6H4 |
577 | Bn | H | Me | H | H | H | H | 1-Naph |
578 | Bn | H | Me | H | H | H | H | 噻吩-2-基 |
579 | Bn | H | Me | H | H | H | H | 吡啶-3-基 |
580 | Bn | H | Me | Me | H | H | H | 4-ClC6H4 |
581 | Bn | H | Et | H | H | H | H | Ph |
582 | Bn | H | Et | H | H | H | H | 2-ClC6H4 |
583 | Bn | H | Et | H | H | H | H | 3-ClC6H4 |
584 | Bn | H | Et | H | H | H | H | 4-ClC6H4 |
585 | Bn | H | Et | H | H | H | H | 4-MeC6H4 |
586 | Bn | H | Et | H | H | H | H | 4-t-BuC6H4 |
587 | Bn | H | Et | H | H | H | H | 1-Naph |
588 | Bn | H | Et | H | H | H | H | 噻吩-2-基 |
589 | Bn | H | Et | H | H | H | H | 4-甲基吡啶-5-基 |
590 | Bn | H | Et | Me | H | H | H | 4-ClC6H4 |
591 | Bn | H | n-Pr | H | H | H | H | Ph |
592 | Bn | H | n-Pr | H | H | H | H | 2-ClC6H4 |
593 | Bn | H | n-Pr | H | H | H | H | 4-ClC6H4 |
594 | Bn | H | n-Pr | H | H | H | H | 4-MeC6H4 |
595 | Bn | H | n-Pr | H | H | H | H | 4-EtC6H4 |
表1-17
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
596 | Bn | H | i-Pr | H | H | H | H | Ph |
597 | Bn | H | i-Pr | H | H | H | H | 4-ClC6H4 |
598 | Bn | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
599 | Bn | H | i-Pr | H | H | H | H | 2-MeC6H4 |
600 | Bn | H | i-Pr | H | H | H | H | 4-MeC6H4 |
601 | Bn | H | i-Pr | H | H | H | H | 4-EtC6H4 |
602 | Bn | H | i-Pr | H | H | H | H | 2-Naph |
603 | Bn | H | i-Pr | H | H | H | H | 5-甲基噻吩-2-基 |
604 | Bn | H | i-Pr | H | H | H | H | 吡啶-3-基 |
605 | Bn | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
606 | Bn | H | s-Bu | H | H | H | H | Ph |
607 | Bn | H | s-Bu | H | H | H | H | 4-ClC6H4 |
608 | Bn | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
609 | Bn | H | s-Bu | H | H | H | H | 2-MeC6H4 |
610 | Bn | H | s-Bu | H | H | H | H | 4-MeC6H4 |
611 | Bn | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
612 | Bn | H | s-Bu | H | H | H | H | 1-Naph |
613 | Bn | H | s-Bu | H | H | H | H | 噻吩-2-基 |
614 | Bn | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
615 | Bn | H | s-Bu | Me | H | H | H | 4-CF3C6H4 |
616 | Bn | H | i-Bu | H | H | H | H | Ph |
617 | Bn | H | i-Bu | H | H | H | H | 4-ClC6H4 |
618 | Bn | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
619 | Bn | H | i-Bu | H | H | H | H | 2-MeC6H4 |
620 | Bn | H | i-Bu | H | H | H | H | 4-MeC6H4 |
621 | Bn | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
622 | Bn | H | i-Bu | H | H | H | H | 2-Naph |
623 | Bn | H | i-Bu | H | H | H | H | 噻吩-2-基 |
624 | Bn | H | i-Bu | H | H | H | H | 3-甲基-异噻唑-5-基 |
625 | Bn | H | i-Bu | Me | H | H | H | 4-ClC6H4 |
626 | Bn | H | t-Bu | H | H | H | H | Ph |
627 | Bn | H | t-Bu | H | H | H | H | 4-ClC6H4 |
628 | Bn | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
629 | Bn | H | t-Bu | H | H | H | H | 2-MeC6H4 |
630 | Bn | H | t-Bu | H | H | H | H | 4-MeC6H4 |
631 | Bn | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
632 | Bn | H | t-Bu | H | H | H | H | 1-Naph |
633 | Bn | H | t-Bu | H | H | H | H | 噻吩-2-基 |
634 | Bn | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
635 | Bn | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
表1-18
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
636 | Bn | H | Ph | H | H | H | H | Ph |
637 | Bn | H | Ph | H | H | H | H | 2-ClC6H4 |
638 | Bn | H | Ph | H | H | H | H | 4-ClC6H4 |
639 | Bn | H | Ph | H | H | H | H | 4-MeC6H4 |
640 | Bn | H | Ph | H | H | H | H | 4-EtC6H4 |
641 | Bn | H | 4-MeC6H4 | H | H | H | H | Ph |
642 | Bn | H | 4-MeC6H4 | H | H | H | H | 4-CF3C6H4 |
643 | Bn | H | 4-MeC6H4 | H | H | H | H | 2-MeC6H4 |
644 | Bn | H | 4-MeC6H4 | H | H | H | H | 4-MeC6H4 |
645 | Bn | H | 4-MeC6H4 | H | H | H | H | 4-t-BuC6H4 |
646 | Bn | H | Bn | H | H | H | H | Ph |
647 | Bn | H | Bn | H | H | H | H | 4-CF3C6H4 |
648 | Bn | H | Bn | H | H | H | H | 2-MeC6H4 |
649 | Bn | H | Bn | H | H | H | H | 4-MeC6H4 |
650 | Bn | H | Bn | H | H | H | H | 4-EtC6H4 |
651 | Bn | H | -(CH2)4- | H | H | H | 4-ClC6H4 | |
652 | Bn | H | -(CH2)5- | H | H | H | 4-ClC6H4 | |
653 | 2-Naph | H | Me | H | H | H | H | Ph |
654 | 2-Naph | H | Me | H | H | H | H | 2-BrC6H4 |
655 | 2-Naph | H | Me | Me | H | H | H | 3-BrC6H4 |
656 | 2-Naph | H | Me | H | H | H | H | 4-BrC6H4 |
657 | 2-Naph | H | Me | H | H | H | H | 4-MeC6H4 |
658 | 2-Naph | H | Me | H | H | H | H | 4-t-BuC6H4 |
659 | 2-Naph | H | Me | H | H | H | H | 1-Naph |
660 | 2-Naph | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
661 | 2-Naph | H | Me | H | H | H | H | 吡啶-3-基 |
662 | 2-Naph | H | Me | Me | H | H | H | 4-ClC6H4 |
663 | 2-Naph | H | Et | H | H | H | H | Ph |
664 | 2-Naph | H | Et | H | H | H | H | 2-FC6H4 |
665 | 2-Naph | H | Et | H | H | H | H | 3-FC6H4 |
666 | 2-Naph | H | Et | H | H | H | H | 4-FC6H4 |
667 | 2-Naph | H | Et | H | H | H | H | 4-MeC6H4 |
68 | 2-Naph | H | Et | H | H | H | H | 4-t-BuC6H4 |
669 | 2-Naph | H | Et | H | H | H | H | 1-Naph |
670 | 2-Naph | H | Et | H | H | H | H | 噻吩-2-基 |
671 | 2-Naph | H | Et | H | H | H | H | 吡啶-3-基 |
672 | 2-Naph | H | Et | Me | H | H | H | 4-ClC6H4 |
表1-19
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
673 | 2-Naph | H | i-Pr | H | H | H | H | Ph |
674 | 2-Naph | H | i-Pr | H | H | H | H | 4-ClC6H4 |
675 | 2-Naph | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
676 | 2-Naph | H | i-Pr | H | H | H | H | 2-MeC6H4 |
677 | 2-Naph | H | i-Pr | H | H | H | H | 4-MeC6H4 |
678 | 2-Naph | H | i-Pr | H | H | H | H | 4-EtC6H4 |
679 | 2-Naph | H | i-Pr | H | H | H | H | 2-Naph |
680 | 2-Naph | H | i-Pr | H | H | H | H | 噻吩-2-基 |
681 | 2-Naph | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
682 | 2-Naph | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
683 | 2-Naph | H | s-Bu | H | H | H | H | Ph |
684 | 2-Naph | H | s-Bu | H | H | H | H | 4-ClC6H4 |
685 | 2-Naph | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
686 | 2-Naph | H | s-Bu | H | H | H | H | 2-MeC6H4 |
687 | 2-Naph | H | s-Bu | H | H | H | H | 4-MeC6H4 |
688 | 2-Naph | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
689 | 2-Naph | H | s-Bu | H | H | H | H | 1-Naph |
690 | 2-Naph | H | s-Bu | H | H | H | H | 噻吩-2-基 |
691 | 2-Naph | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
692 | 2-Naph | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
693 | 2-Naph | H | i-Bu | H | H | H | H | Ph |
694 | 2-Naph | H | i-Bu | H | H | H | H | 4-ClC6H4 |
695 | 2-Naph | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
696 | 2-Naph | H | i-Bu | H | H | H | H | 2-MeC6H4 |
697 | 2-Naph | H | i-Bu | H | H | H | H | 4-MeC6H4 |
698 | 2-Naph | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
699 | 2-Naph | H | i-Bu | H | H | H | H | 1-Naph |
700 | 2-Naph | H | i-Bu | H | H | H | H | 噻吩-2-基 |
701 | 2-Naph | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
702 | 2-Naph | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
703 | 2-Naph | H | c-Hex | H | H | H | H | Ph |
704 | 2-Naph | H | c-Hex | H | H | H | H | 4-ClC6H4 |
705 | 2-Naph | H | c-Hex | H | H | H | H | 3,4-Cl2C6H3 |
706 | 2-Naph | H | c-Hex | H | H | H | H | 2-MeC6H4 |
707 | 2-Naph | H | c-Hex | H | H | H | H | 4-MeC6H4 |
708 | 2-Naph | H | c-Hex | H | H | H | H | 4-t-BuC6H4 |
709 | 2-Naph | H | c-Hex | H | H | H | H | 1-Naph |
710 | 2-Naph | H | c-Hex | H | H | H | H | 噻吩-2-基 |
711 | 2-Naph | H | c-Hex | H | H | H | H | 异噻唑-5-基 |
712 | 2-Naph | H | c-Hex | Me | H | H | H | 4-MeC6H4 |
表1-20
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
713 | 2-Naph | H | Ph | H | H | H | H | Ph |
714 | 2-Naph | H | ph | H | H | H | H | 2-ClC6H4 |
715 | 2-Naph | H | Ph | H | H | H | H | 4-ClC6H4 |
716 | 2-Naph | H | Ph | H | H | H | H | 4-MeC6H4 |
717 | 2-Naph | H | Ph | H | H | H | H | 4-EtC6H4 |
718 | 烯丙基 | H | Me | H | H | H | H | Ph |
719 | 烯丙基 | H | Me | H | H | H | H | 2-ClC6H4 |
720 | 烯丙基 | H | Me | Me | H | H | H | 3-ClC6H4 |
721 | 烯丙基 | H | Me | H | H | H | H | 4-ClC6H4 |
722 | 烯丙基 | H | Me | H | H | H | H | 4-CNC6H4 |
723 | 烯丙基 | H | Me | H | H | H | H | 4-t-BuC6H4 |
724 | 烯丙基 | H | Me | H | H | H | H | 1-Naph |
725 | 烯丙基 | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
726 | 烯丙基 | H | Me | H | H | H | H | 吡啶-3-基 |
727 | 烯丙基 | H | Me | Me | H | H | H | 4-CF3C6H4 |
728 | 烯丙基 | H | Et | H | H | H | H | Ph |
729 | 烯丙基 | H | Et | H | H | H | H | 2-ClC6H4 |
730 | 烯丙基 | H | Et | H | H | H | H | 3-ClC6H4 |
731 | 烯丙基 | H | Et | H | H | H | H | 4-ClC6H4 |
732 | 烯丙基 | H | Et | H | H | H | H | 4-MeC6H4 |
733 | 烯丙基 | H | Et | H | H | H | H | 4-t-BuC6H4 |
734 | 烯丙基 | H | Et | H | H | H | H | 1-Naph |
735 | 烯丙基 | H | Et | H | H | H | H | 噻吩-2-基 |
736 | 烯丙基 | H | Et | H | H | H | H | 吡啶-3-基 |
737 | 烯丙基 | H | Et | Me | H | H | H | 4-ClC6H4 |
738 | 烯丙基 | H | i-Pr | H | H | H | H | Ph |
739 | 烯丙基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
740 | 烯丙基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
741 | 烯内基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
742 | 烯丙基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
743 | 烯丙基 | H | i-Pr | H | H | H | H | 4-EtC6H4 |
744 | 烯丙基 | H | i-Pr | H | H | H | H | 2-Naph |
745 | 烯内基 | H | i-Pr | H | H | H | H | 噻吩-2-基 |
746 | 烯丙基 | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
747 | 烯丙基 | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
表1-21
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
748 | 烯丙基 | H | s-Bu | H | H | H | H | Ph |
749 | 烯丙基 | H | s-Bu | H | H | H | H | 4-ClC6H4 |
750 | 烯丙基 | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
751 | 烯丙基 | H | s-Bu | H | H | H | H | 2-MeC6H4 |
752 | 烯丙基 | H | s-Bu | H | H | H | H | 4-MeC6H4 |
753 | 烯丙基 | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
754 | 烯丙基 | H | s-Bu | H | H | H | H | 1-Naph |
755 | 烯丙基 | H | s-Bu | H | H | H | H | 噻吩-2-基 |
756 | 烯丙基 | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
757 | 烯丙基 | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
758 | 烯丙基 | H | i-Bu | H | H | H | H | Ph |
759 | 烯丙基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
760 | 烯丙基 | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
761 | 烯丙基 | H | i-Bu | H | H | H | H | 2-MeC6H4 |
762 | 烯丙基 | H | i-Bu | H | H | H | H | 4-MeC6H4 |
763 | 烯丙基 | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
764 | 烯丙基 | H | i-Bu | H | H | H | H | 1-Naph |
765 | 烯丙基 | H | i-Bu | H | H | H | H | 噻吩-2-基 |
766 | 烯丙基 | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
767 | 烯丙基 | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
768 | 烯丙基 | H | t-Bu | H | H | H | H | Ph |
769 | 烯丙基 | H | t-Bu | H | H | H | H | 4-ClC6H4 |
770 | 烯丙基 | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
771 | 烯丙基 | H | t-Bu | H | H | H | H | 2-MeC6H4 |
772 | 烯丙基 | H | t-Bu | H | H | H | H | 4-MeC6H4 |
773 | 烯丙基 | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
774 | 烯丙基 | H | t-Bu | H | H | H | H | 1-Naph |
775 | 烯丙基 | H | t-Bu | H | H | H | H | 噻吩-2-基 |
776 | 烯丙基 | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
777 | 烯丙基 | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
778 | 烯丙基 | H | Ph | H | H | H | H | Ph |
779 | 烯丙基 | H | Ph | H | H | H | H | 2-ClC6H4 |
780 | 烯丙基 | H | 4-FC6H4 | H | H | H | H | 4-ClC6H4 |
781 | 烯丙基 | H | Ph | H | H | H | H | 4-MeC6H4 |
782 | 烯丙基 | H | 4-BrC6H4 | H | H | H | H | 4-EtC6H4 |
表1-22
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
783 | 炔丙基 | H | Me | H | H | H | H | Ph |
784 | 炔丙基 | H | Me | H | H | H | H | 2-IC6H4 |
785 | 炔丙基 | H | Me | H | Me | Me | H | 3-IC6H4 |
786 | 炔丙基 | H | Me | H | H | H | H | 4-IC6H4 |
787 | 炔丙基 | H | Me | H | H | H | H | 4-MeC6H4 |
788 | 炔丙基 | H | Me | H | H | H | H | 4-t-BuC6H4 |
789 | 炔丙基 | H | Me | H | H | H | H | 1-Naph |
790 | 炔丙基 | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
791 | 炔丙基 | H | Me | H | H | H | H | 吡啶-3-基 |
792 | 炔丙基 | H | Me | Me | H | H | H | 4-ClC6H4 |
793 | 炔丙基 | H | Et | H | H | H | H | Ph |
794 | 炔丙基 | H | Et | H | H | H | H | 2-ClC6H4 |
795 | 炔丙基 | H | Et | H | H | H | H | 3-ClC6H4 |
796 | 炔丙基 | H | Et | H | H | H | H | 4-ClC6H4 |
797 | 炔丙基 | H | Et | H | H | H | H | 4-MeC6H4 |
798 | 炔丙基 | H | Et | H | H | H | H | 4-t-BuC6H4 |
799 | 炔丙基 | H | Et | H | H | H | H | 1-Naph |
800 | 炔丙基 | H | Et | H | H | H | H | 噻吩-2-基 |
801 | 炔丙基 | H | Et | H | H | H | H | 吡啶-3-基 |
802 | 炔丙基 | H | Et | Me | H | H | H | 4-ClC6H4 |
803 | 炔丙基 | H | i-Pr | H | H | H | H | Ph |
804 | 炔丙基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
805 | 炔丙基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
806 | 炔丙基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
807 | 炔丙基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
808 | 炔丙基 | H | i-Pr | H | H | H | H | 4-EtC6H4 |
809 | 炔丙基 | H | i-Pr | H | H | H | H | 2-Naph |
810 | 炔丙基 | H | i-Pr | H | H | H | H | 噻吩-2-基 |
811 | 炔丙基 | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
812 | 炔丙基 | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
813 | 炔丙基 | H | s-Bu | H | H | H | H | Ph |
814 | 炔丙基 | H | s-Bu | H | H | H | H | 4-ClC6H4 |
815 | 炔丙基 | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
816 | 炔丙基 | H | s-Bu | H | H | H | H | 2-MeC6H4 |
817 | 炔丙基 | H | s-Bu | H | H | H | H | 4-MeC6H4 |
818 | 炔丙基 | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
819 | 炔丙基 | H | s-Bu | H | H | H | H | 1-Naph |
820 | 炔丙基 | H | s-Bu | H | H | H | H | 噻吩-2-基 |
821 | 炔丙基 | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
表1-23
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
822 | 炔丙基 | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
823 | 炔丙基 | H | i-Bu | H | H | H | H | Ph |
824 | 炔丙基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
825 | 炔丙基 | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
826 | 炔丙基 | H | i-Bu | H | H | H | H | 2-MeC6H4 |
827 | 炔丙基 | H | i-Bu | H | H | H | H | 4-MeC6H4 |
828 | 炔丙基 | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
829 | 炔丙基 | H | i-Bu | H | H | H | H | 1-Naph |
830 | 炔丙基 | H | i-Bu | H | H | H | H | 噻吩-2-基 |
831 | 炔丙基 | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
832 | 炔丙基 | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
833 | 炔丙基 | H | t-Bu | H | H | H | H | Ph |
834 | 炔丙基 | H | t-Bu | H | H | H | H | 4-ClC6H4 |
835 | 炔丙基 | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
836 | 炔丙基 | H | t-Bu | H | H | H | H | 2-MeC6H4 |
837 | 炔丙基 | H | t-Bu | H | H | H | H | 4-MeC6H4 |
838 | 炔丙基 | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
839 | 炔丙基 | H | t-Bu | H | H | H | H | 1-Naph |
840 | 炔丙基 | H | t-Bu | H | H | H | H | 噻吩-2-基 |
841 | 炔丙基 | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
842 | 炔丙基 | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
843 | 炔丙基 | H | Ph | H | H | H | H | Ph |
844 | 炔丙基 | H | Ph | H | H | H | H | 2-ClC6H4 |
845 | 炔丙基 | H | 4-ClC6H4 | H | H | H | H | 4-ClC6H4 |
846 | 炔丙基 | H | Ph | H | H | H | H | 4-MeC6H4 |
847 | 炔丙基 | H | 4-MeC6H4 | H | H | H | H | 4-EtC6H4 |
848 | c-Pr | H | Me | H | H | H | H | Ph |
849 | c-Pr | H | Me | H | H | H | H | 2-ClC6H4 |
850 | c-Pr | H | Me | Me | H | H | H | 3-ClC6H4 |
851 | c-Pr | H | Me | H | H | H | H | 4-ClC6H4 |
852 | c-Pr | H | Me | H | H | H | H | 4-MeC6H4 |
853 | c-Pr | H | Me | H | H | H | H | 4-t-BuC6H4 |
854 | c-Pr | H | Me | H | H | H | H | 1-Naph |
855 | c-Pr | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
856 | c-Pr | H | Me | H | H | H | H | 吡啶-3-基 |
857 | c-Pr | H | Me | Me | H | H | H | 4-ClC6H4 |
表1-24
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
858 | c-Pr | H | Et | H | H | H | H | Ph |
859 | c-Pr | H | Et | H | H | H | H | 2-ClC6H4 |
860 | c-Pr | H | Et | H | H | H | H | 3-ClC6H4 |
861 | c-Pr | H | Et | H | H | H | H | 4-ClC6H4 |
862 | c-Pr | H | Et | H | H | H | H | 4-MeC6H4 |
863 | c-Pr | H | Et | H | H | H | H | 4-t-BuC6H4 |
864 | c-Pr | H | Et | H | H | H | H | 1-Naph |
865 | c-Pr | H | Et | H | H | H | H | 噻吩-2-基 |
866 | c-Pr | H | Et | H | H | H | H | 吡啶-3-基 |
867 | c-Pr | H | Et | Me | H | H | H | 4-ClC6H4 |
868 | c-Pr | H | i-Pr | H | H | H | H | Ph |
869 | c-Pr | H | i-Pr | H | H | H | H | 4-ClC6H4 |
870 | c-Pr | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
871 | c-Pr | H | i-Pr | H | H | H | H | 2-MeC6H4 |
872 | c-Pr | H | i-Pr | H | H | H | H | 4-MeC6H4 |
873 | c-Pr | H | i-Pr | H | H | H | H | 4-EtC6H4 |
874 | c-Pr | H | i-Pr | H | H | H | H | 2-Naph |
875 | c-Pr | H | i-Pr | H | H | H | H | 噻吩-2-基 |
876 | c-Pr | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
878 | c-Pr | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
879 | c-Pr | H | s-Bu | H | H | H | H | Ph |
880 | c-Pr | H | s-Bu | H | H | H | H | 4-ClC6H4 |
881 | c-Pr | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
882 | c-Pr | H | s-Bu | H | H | H | H | 2-MeC6H4 |
883 | c-Pr | H | s-Bu | H | H | H | H | 4-MeC6H4 |
884 | c-Pr | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
885 | c-Pr | H | s-Bu | H | H | H | H | 1-Naph |
886 | c-Pr | H | s-Bu | H | H | H | H | 噻吩-2-基 |
887 | c-Pr | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
888 | c-Pr | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
889 | c-Pr | H | i-Bu | H | H | H | H | Ph |
890 | c-Pr | H | i-Bu | H | H | H | H | 4-ClC6H4 |
891 | c-Pr | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
892 | c-Pr | H | i-Bu | H | H | H | H | 2-MeC6H4 |
893 | c-Pr | H | i-Bu | H | H | H | H | 4-MeC6H4 |
894 | c-Pr | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
895 | c-Pr | H | i-Bu | H | H | H | H | 1-Naph |
896 | c-Pr | H | i-Bu | H | H | H | H | 噻吩-2-基 |
897 | c-Pr | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
898 | c-Pr | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
表1-25
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
899 | c-Pr | H | t-Bu | H | Bn | H | H | Ph |
900 | c-Pr | H | t-Bu | H | H | H | H | 4-ClC6H4 |
901 | c-Pr | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
902 | c-Pr | H | t-Bu | H | H | H | H | 2-MeC6H4 |
903 | c-Pr | H | t-Bu | H | H | H | H | 4-MeC6H4 |
904 | c-Pr | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
905 | c-Pr | H | t-Bu | H | H | H | H | 1-Naph |
906 | c-Pr | H | t-Bu | H | H | H | H | 噻吩-2-基 |
907 | c-Pr | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
908 | c-Pr | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
909 | c-Pr | H | Ph | H | H | H | H | Ph |
910 | c-Pr | H | Ph | H | H | H | H | 2-ClC6H4 |
911 | c-Pr | H | Ph | H | H | H | H | 4-ClC6H4 |
912 | c-Pr | H | Ph | H | H | H | H | 4-MeC6H4 |
913 | c-Pr | H | Ph | H | H | H | H | 4-EtC6H4 |
914 | c-Hex | H | Me | H | H | H | H | Ph |
915 | c-Hex | H | Me | H | H | H | H | 2-ClC6H4 |
916 | c-Hex | H | Me | H | Et | H | H | 3-ClC6H4 |
917 | c-Hex | H | Me | H | H | H | H | 4-ClC6H4 |
918 | c-Hex | H | Me | H | H | H | H | 4-MeC6H4 |
919 | c-Hex | H | Me | H | H | H | H | 4-t-BuC6H4 |
920 | c-Hex | H | Me | H | H | H | H | 1-Naph |
921 | c-Hex | H | Me | H | H | H | H | 5-甲基噻吩-2-基 |
922 | c-Hex | H | Me | H | H | H | H | 吡啶-3-基 |
923 | c-Hex | H | Me | Me | H | H | H | 4-ClC6H4 |
924 | c-Hex | H | Et | H | H | H | H | Ph |
925 | c-Hex | H | Et | H | H | H | H | 2-ClC6H4 |
926 | c-Hex | H | Et | H | H | H | H | 3-ClC6H4 |
927 | c-Hex | H | Et | H | H | H | H | 4-ClC6H4 |
928 | c-Hex | H | Et | H | H | H | H | 4-MeC6H4 |
929 | c-Hex | H | Et | H | H | H | H | 4-t-BuC6H4 |
930 | c-Hex | H | Et | H | H | H | H | 1-Naph |
931 | c-Hex | H | Et | H | H | H | H | 噻吩-2-基 |
932 | c-Hex | H | Et | H | H | H | H | 吡啶-3-基 |
933 | c-Hex | H | Et | Me | H | H | H | 4-ClC6H4 |
表1-26
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
934 | c-Hex | H | i-Pr | H | H | H | H | Ph |
935 | c-Hex | H | i-Pr | H | H | H | H | 4-ClC6H4 |
936 | c-Hex | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
937 | c-Hex | H | i-Pr | H | H | H | H | 2-MeC6H4 |
938 | c-Hex | H | i-Pr | H | H | H | H | 4-MeC6H4 |
939 | c-Hex | H | i-Pr | H | H | H | H | 4-EtC6H4 |
940 | c-Hex | H | i-Pr | H | H | H | H | 2-Naph |
941 | c-Hex | H | i-Pr | H | H | H | H | 噻吩-2-基 |
942 | c-Hex | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
943 | c-Hex | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
944 | c-Hex | H | s-Bu | H | H | H | H | Ph |
945 | c-Hex | H | s-Bu | H | H | H | H | 4-ClC6H4 |
946 | c-Hex | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
947 | c-Hex | H | s-Bu | H | H | H | H | 2-MeC6H4 |
948 | c-Hex | H | s-Bu | H | H | H | H | 4-MeC6H4 |
949 | c-Hex | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
950 | c-Hex | H | s-Bu | H | Ph | H | H | 1-Naph |
951 | c-Hex | H | s-Bu | H | H | H | H | 噻吩-2-基 |
952 | c-Hex | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
953 | c-Hex | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
954 | c-Hex | H | i-Bu | H | H | H | H | Ph |
955 | c-Hex | H | i-Bu | H | H | H | H | 4-ClC6H4 |
956 | c-Hex | H | i-Bu | H | H | H | H | 3,4-Cl2C6H3 |
957 | c-Hex | H | i-Bu | H | H | H | H | 2-MeC6H4 |
958 | c-Hex | H | i-Bu | H | H | H | H | 4-MeC6H4 |
959 | c-Hex | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
960 | c-Hex | H | i-Bu | H | H | H | H | 1-Naph |
961 | c-Hex | H | i-Bu | H | H | H | H | 噻吩-2-基 |
962 | c-Hex | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
963 | c-Hex | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
964 | c-Hex | H | t-Bu | H | H | H | H | Ph |
965 | c-Hex | H | t-Bu | H | H | H | H | 4-ClC6H4 |
966 | c-Hex | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
967 | c-Hex | H | t-Bu | H | H | H | H | 2-MeC6H4 |
968 | c-Hex | H | t-Bu | H | H | H | H | 4-MeC6H4 |
969 | c-Hex | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
970 | c-Hex | H | t-Bu | H | H | H | H | 1-Naph |
971 | c-Hex | H | t-Bu | H | H | H | H | 噻吩-2-基 |
972 | c-Hex | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
973 | c-Hex | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
表1-27
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
974 | c-Hex | H | Ph | H | H | H | H | Ph |
975 | c-Hex | H | Ph | H | H | H | H | 2-ClC6H4 |
976 | c-Hex | H | Ph | H | H | H | H | 4-ClC6H4 |
977 | c-Hex | H | Ph | H | H | H | H | 4-MeC6H4 |
978 | c-Hex | H | Ph | H | H | H | H | 4-EtC6H4 |
979 | 乙烯基 | H | Me | H | H | H | H | Ph |
980 | 乙烯基 | H | Me | H | H | H | H | 2-ClC6H4 |
981 | 乙烯基 | H | Me | Me | H | H | H | 3-ClC6H4 |
982 | 乙烯基 | H | Me | H | H | H | H | 4-ClC6H4 |
983 | 乙烯基 | H | Me | H | H | H | H | 4-MeC6H4 |
984 | 乙烯基 | H | Me | H | H | H | H | 4-t-BuC6H4 |
985 | 乙烯基 | H | Me | H | H | H | H | 1-Naph |
986 | 乙烯基 | H | Me | H | H | H | H | 5-乙基噻吩-2-基 |
987 | 乙烯基 | H | Me | H | H | H | H | 吡啶-3-基 |
988 | 乙烯基 | H | Me | Me | H | H | H | 4-ClC6H4 |
989 | 乙烯基 | H | Et | H | H | H | H | Ph |
990 | 乙烯基 | H | Et | H | H | H | H | 2-ClC6H4 |
991 | 乙烯基 | H | Et | H | H | H | H | 3-ClC6H4 |
992 | 乙烯基 | H | Et | H | H | H | H | 4-ClC6H4 |
993 | 乙烯基 | H | Et | H | H | H | H | 4-MeC6H4 |
994 | 乙烯基 | H | Et | H | H | H | H | 4-t-BuC6H4 |
995 | 乙烯基 | H | Et | H | H | H | H | 1-Naph |
996 | 乙烯基 | H | Et | H | H | H | H | 噻吩-2-基 |
997 | 乙烯基 | H | Et | H | H | H | H | 吡啶-3-基 |
998 | 乙烯基 | H | Et | Me | H | H | H | 4-ClC6H4 |
999 | 乙烯基 | H | i-Pr | H | H | H | H | Ph |
1000 | 乙烯基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1001 | 乙烯基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1002 | 乙烯基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1003 | 乙烯基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1004 | 乙烯基 | H | i-Pr | H | H | H | H | 4-EtC6H4 |
1005 | 乙烯基 | H | i-Pr | H | H | H | H | 2-Naph |
1006 | 乙烯基 | H | i-Pr | H | H | H | H | 噻吩-2-基 |
1007 | 乙烯基 | H | i-Pr | H | H | H | H | 5-甲基吡啶-3-基 |
1008 | 乙烯基 | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
表1-28
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1009 | 乙烯基 | H | s-Bu | H | H | H | H | 4-ClC6H4 |
1010 | 乙烯基 | H | s-Bu | H | H | H | H | 3,4-Cl2C6H3 |
1011 | 乙烯基 | H | s-Bu | H | H | H | H | 2-MeC6H4 |
1012 | 乙烯基 | H | s-Bu | H | H | H | H | 4-MeC6H4 |
1013 | 乙烯基 | H | s-Bu | H | H | H | H | 4-t-BuC6H4 |
1014 | 乙烯基 | H | s-Bu | H | H | H | H | 1-Naph |
1015 | 乙烯基 | H | s-Bu | H | H | H | H | 噻吩-2-基 |
1016 | 乙烯基 | H | s-Bu | H | H | H | H | 异噻唑-5-基 |
1017 | 乙烯基 | H | s-Bu | Me | H | H | H | 4-MeC6H4 |
1018 | 乙烯基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1019 | 乙烯基 | H | i-Bu | H | Ph | H | H | 3,4-Cl2C6H3 |
1020 | 乙烯基 | H | i-Bu | H | H | H | H | 2-MeC6H4 |
1021 | 乙烯基 | H | i-Bu | H | H | H | H | 4-MeC6H4 |
1022 | 乙烯基 | H | i-Bu | H | H | H | H | 4-t-BuC6H4 |
1023 | 乙烯基 | H | i-Bu | H | H | H | H | 1-Naph |
1024 | 乙烯基 | H | i-Bu | H | H | H | H | 噻吩-2-基 |
1025 | 乙烯基 | H | i-Bu | H | H | H | H | 异噻唑-5-基 |
1026 | 乙烯基 | H | i-Bu | Me | H | H | H | 4-MeC6H4 |
1027 | 乙烯基 | H | t-Bu | H | H | H | H | Ph |
1028 | 乙烯基 | H | t-Bu | H | H | H | H | 4-ClC6H4 |
1029 | 乙烯基 | H | t-Bu | H | H | H | H | 3,4-Cl2C6H3 |
1030 | 乙烯基 | H | t-Bu | H | H | H | H | 2-MeC6H4 |
1031 | 乙烯基 | H | t-Bu | H | H | H | H | 4-MeC6H4 |
1032 | 乙烯基 | H | t-Bu | H | H | H | H | 4-t-BuC6H4 |
1033 | 乙烯基 | H | t-Bu | H | H | H | H | 1-Naph |
1034 | 乙烯基 | H | t-Bu | H | H | H | H | 噻吩-2-基 |
1035 | 乙烯基 | H | t-Bu | H | H | H | H | 异噻唑-5-基 |
1036 | 乙烯基 | H | t-Bu | Me | H | H | H | 4-MeC6H4 |
1037 | 乙烯基 | H | Ph | H | H | H | H | Ph |
1038 | 乙烯基 | H | Ph | H | H | H | H | 2-ClC6H4 |
1039 | 乙烯基 | H | Ph | H | H | H | H | 4-ClC6H4 |
1040 | 乙烯基 | H | Ph | H | H | H | H | 4-MeC6H4 |
1041 | 乙烯基 | H | Ph | H | H | H | H | 4-EtC6H4 |
1042 | 4-MeC6H4CH2 | H | Me | H | H | H | H | Ph |
1043 | 4-MeC6H4CH2 | H | Me | H | H | H | H | 2-BrC6H4 |
1044 | 4-MeC6H4CH2 | H | Me | H | H | H | H | 3-BrC6H4 |
1045 | 4-MeC6H4CH2 | H | Me | H | H | H | H | 4-BrC6H4 |
1046 | 4-MeC6H4CH2 | H | Me | H | H | H | H | 4-MeC6H4 |
表1-29
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1047 | 4-MeC6H4CH2 | H | i-Pr | H | H | H | H | 2-ClC6H4 |
1048 | 4-MeC6H4CH2 | H | i-Pr | H | H | H | H | 3-ClC6H4 |
1049 | 4-MeC6H4CH2 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1050 | 4-MeC6H4CH2 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1051 | 4-MeC6H4CH2 | H | i-Pr | H | H | H | H | 4-EtC6H4 |
1052 | 4-MeC6H4CH2 | H | i-Bu | H | H | H | H | Ph |
1053 | 4-MeC6H4CH2 | H | i-Bu | H | H | H | H | 2-FC6H4 |
1054 | 4-MeC6H4CH2 | H | i-Bu | H | H | H | H | 3-FC6H4 |
1055 | 4-MeC6H4CH2 | H | i-Bu | H | H | H | H | 4-FC6H4 |
1056 | 4-MeC6H4CH2 | H | i-Bu | H | H | H | H | 4-MeC6H4 |
1057 | 4-ClC6H4CH2 | H | Me | H | H | H | H | Ph |
1058 | 4-ClC6H4CH2 | H | Me | H | H | H | H | 4-ClC6H4 |
1059 | 4-ClC6H4CH2 | H | Me | H | H | H | H | 4-MeC6H4 |
1060 | 4-ClC6H4CH2 | H | Me | H | H | H | H | 噻吩-2-基 |
1061 | 4-ClC6H4CH2 | H | Me | H | H | H | H | 吡啶-3-基 |
1062 | 4-ClC6H4CH2 | H | i-Pr | H | H | H | H | Ph |
1063 | 4-ClC6H4CH2 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1064 | 4-ClC6H4CH2 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1065 | 4-ClC6H4CH2 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1066 | 4-ClC6H4CH2 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1067 | 4-ClC6H4CH2 | H | i-Bu | H | H | H | H | Ph |
1068 | 4-ClC6H4CH2 | H | i-Bu | H | H | H | H | 2-MeC6H4 |
1069 | 4-ClC6H4CH2 | H | i-Bu | H | H | H | H | 3-MeC6H4 |
1070 | 4-ClC6H4CH2 | H | i-Bu | H | H | H | H | 4-MeC6H4 |
1071 | 4-ClC6H4CH2 | H | i-Bu | Me | H | H | H | 1-Naph |
1072 | PhCH(CH3) | H | Me | H | H | H | H | Ph |
1073 | PhCH(CH3) | H | Me | H | H | H | H | 4-ClC6H4 |
1074 | PhCH(CH3) | H | Me | H | H | H | H | 4-MeC6H4 |
1075 | PhCH(CH3) | H | Me | H | H | H | H | 噻吩-2-基 |
1076 | PhCH(CH3) | H | Me | H | H | H | H | 吡啶-4-基 |
1077 | PhCH(CH3) | H | i-Pr | H | H | H | H | Ph |
1078 | PhCH(CH3) | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1079 | PhCH(CH3) | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1080 | PhCH(CH3) | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1081 | PhCH(CH3) | H | i-Pr | Me | H | H | H | 4-MeC6H4 |
1082 | PhCH(CH3) | H | i-Bu | H | H | H | H | Ph |
1083 | PhCH(CH3) | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1084 | PhCH(CH3) | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1085 | PhCH(CH3) | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1086 | PhCH(CH3) | H | i-Bu | Me | H | H | H | 1-Naph |
表1-30
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1087 | PhCH(i-Pr) | H | Me | H | H | H | H | Ph |
1088 | PhCH(i-Pr) | H | Me | H | H | H | H | 4-ClC6H4 |
1089 | PhCH(i-Pr) | H | Me | H | H | H | H | 4-MeC6H4 |
1090 | PhCH(i-Pr) | H | Me | H | H | H | H | 噻吩-2-基 |
1091 | PhCH(i-Pr) | H | Me | H | H | H | H | 吡啶-2-基 |
1092 | PhCH(i-Pr) | H | i-Pr | H | H | H | H | Ph |
1093 | PhCH(i-Pr) | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1094 | PhCH(i-Pr) | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1095 | PhCH(i-Pr) | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1096 | PhCH(i-Pr) | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1097 | PhCH(i-Pr) | H | i-Bu | H | H | H | H | Ph |
1098 | PhCH(i-Pr) | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1099 | PhCH(i-Pr) | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1100 | PhCH(i-Pr) | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1101 | PhCH(i-Pr) | H | i-Bu | H | H | H | H | 1-Naph |
1102 | PhC(CH3)2 | H | Me | H | H | H | H | Ph |
1103 | PhC(CH3)2 | H | Me | H | H | H | H | 4-ClC6H4 |
1104 | PhC(CH3)2 | H | Me | H | H | H | H | 4-MeC6H4 |
1105 | PhC(CH3)2 | H | Me | H | H | H | H | 呋喃-2-基 |
1106 | PhC(CH3)2 | H | Me | H | H | H | H | 吡啶-4-基 |
1107 | PhC(CH3)2 | H | i-Pr | H | H | H | H | Ph |
1108 | PhC(CH3)2 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1109 | PhC(CH3)2 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1110 | PhC(CH3)2 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1111 | PhC(CH3)2 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1112 | PhC(CH3)2 | H | i-Bu | H | H | H | H | Ph |
1113 | PhC(CH3)2 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1114 | PhC(CH3)2 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1115 | PhC(CH3)2 | H | i-Bu | H | H | H | H | 4-C1C6H4 |
1116 | PhC(CH3)2 | H | i-Bu | H | H | H | H | 2-Naph |
表1-31
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1117 | 2-呋喃甲基 | H | Me | H | H | H | H | Ph |
1118 | 2-呋喃甲基 | H | Me | H | H | H | H | 4-ClC6H4 |
1119 | 2-呋喃甲基 | H | Me | H | H | H | H | 4-MeC6H4 |
1120 | 2-呋喃甲基 | H | Me | H | H | H | H | 噻吩-2-基 |
1121 | 2-呋喃甲基 | H | Me | H | H | H | H | 吡啶-2-基 |
1122 | 2-呋喃甲基 | H | i-Pr | H | H | H | H | Ph |
1123 | 2-呋喃甲基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1124 | 2-呋喃甲基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1125 | 2-呋喃甲基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1126 | 2-呋喃甲基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1127 | 2-呋喃甲基 | H | i-Bu | H | H | H | H | Ph |
1128 | 2-呋喃甲基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1129 | 2-呋喃甲基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1130 | 2-呋喃甲基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1131 | 2-呋喃甲基 | H | i-Bu | H | H | H | H | 1-Naph |
1132 | 3-呋喃甲基 | H | Me | H | H | H | H | Ph |
1133 | 3-呋喃甲基 | H | Me | H | H | H | H | 4-ClC6H4 |
1134 | 3-呋喃甲基 | H | Me | H | H | H | H | 4-MeC6H4 |
1135 | 3-呋喃甲基 | H | Me | H | H | H | H | 呋喃-2-基 |
1136 | 3-呋喃甲基 | H | Me | H | H | H | H | 吡啶-3-基 |
1137 | 3-呋喃甲基 | H | i-Pr | H | H | H | H | Ph |
1138 | 3-呋喃甲基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1139 | 3-呋喃甲基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1140 | 3-呋喃甲基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1141 | 3-呋喃甲基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1142 | 3-呋喃甲基 | H | i-Bu | H | H | H | H | Ph |
1143 | 3-呋喃甲基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1144 | 3-呋喃甲基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1145 | 3-呋喃甲基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1146 | 3-呋喃甲基 | H | i-Bu | H | H | H | H | 2-Naph |
表1-32
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1147 | 2-四氢呋喃甲基 | H | Me | H | H | H | H | Ph |
1148 | 2-四氢呋喃甲基 | H | Me | H | H | H | H | 4-ClC6H4 |
1149 | 2-四氢呋喃甲基 | H | Me | H | H | H | H | 4-MeC6H4 |
1150 | 2-四氢呋喃甲基 | H | Me | H | H | H | H | 噻吩-2-基 |
1151 | 2-四氢呋喃甲基 | H | Me | H | H | H | H | 吡啶-2-基 |
1152 | 2-四氢呋喃甲基 | H | i-Pr | H | H | H | H | Ph |
1153 | 2-四氢呋喃甲基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1154 | 2-四氢呋喃甲基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1155 | 2-四氢呋喃甲基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1156 | 2-四氢呋喃甲基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1157 | 2-四氢呋喃甲基 | H | i-Bu | H | H | H | H | Ph |
1158 | 2-四氢呋喃甲基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1159 | 2-四氢呋喃甲基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1160 | 2-四氢呋喃甲基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1161 | 2-四氢呋喃甲基 | H | i-Bu | H | H | H | H | 1-Naph |
表1-33
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1162 | 2-噻吩基甲基 | H | Me | H | H | H | H | Ph |
1163 | 2-噻吩基甲基 | H | Me | H | H | H | H | 4-ClC6H4 |
1164 | 2-噻吩基甲基 | H | Me | H | H | H | H | 4-MeC6H4 |
1165 | 2-噻吩基甲基 | H | Me | H | H | H | H | 噻吩-2-基 |
1166 | 2-噻吩基甲基 | H | Me | H | H | H | H | 吡啶-2-基 |
1167 | 2-噻吩基甲基 | H | i-Pr | H | H | H | H | Ph |
1168 | 2-噻吩基甲基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1169 | 2-噻吩基甲基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1170 | 2-噻吩基甲基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1171 | 2-噻吩基甲基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1172 | 2-噻吩基甲基 | H | i-Bu | H | H | H | H | Ph |
1173 | 2-噻吩基甲基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1174 | 2-噻吩基甲基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1175 | 2-噻吩基甲基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1176 | 2-噻吩基甲基 | H | i-Bu | H | H | H | H | 1-Naph |
1177 | 环丙基甲基 | H | Me | H | H | H | H | Ph |
1178 | 环丙基甲基 | H | Me | H | H | H | H | 4-ClC6H4 |
1179 | 环丙基甲基 | H | Me | H | H | H | H | 4-MeC6H4 |
1180 | 环丙基甲基 | H | Me | H | H | H | H | 呋喃-2-基 |
1181 | 环丙基甲基 | H | Me | H | H | H | H | 吡啶-4-基 |
1182 | 环丙基甲基 | H | i-Pr | H | H | H | H | Ph |
1183 | 环丙基甲基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1184 | 环丙基甲基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1185 | 环丙基甲基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1186 | 环丙基甲基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1187 | 环丙基甲基 | H | i-Bu | H | H | H | H | Ph |
1188 | 环丙基甲基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1189 | 环丙基甲基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1190 | 环丙基甲基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1191 | 环丙基甲基 | H | i-Bu | H | H | H | H | 2-Naph |
表1-34
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1192 | 新戊基 | H | Me | H | H | H | H | Ph |
1193 | 新戊基 | H | Me | H | H | H | H | 4-ClC6H4 |
1194 | 新戊基 | H | Me | H | H | H | H | 4-MeC6H4 |
1195 | 新戊基 | H | Me | H | H | H | H | 噻吩-2-基 |
1196 | 新戊基 | H | Me | H | H | H | H | 吡啶-2-基 |
1197 | 新戊基 | H | i-Pr | H | H | H | H | Ph |
1198 | 新戊基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1199 | 新戊基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1200 | 新戊基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1201 | 新戊基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1202 | 新戊基 | H | i-Bu | H | H | H | H | Ph |
1203 | 新戊基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1204 | 新戊基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1205 | 新戊基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1206 | 新戊基 | H | i-Bu | H | H | H | H | 1-Naph |
1207 | 甲代烯丙基 | H | Me | H | H | H | H | Ph |
1208 | 甲代烯丙基 | H | Me | H | H | H | H | 4-ClC6H4 |
1209 | 甲代烯丙基 | H | Me | H | H | H | H | 4-MeC6H4 |
1210 | 甲代烯丙基 | H | Me | H | H | H | H | 呋喃-2-基 |
1211 | 甲代烯丙基 | H | Me | H | H | H | H | 吡啶-4-基 |
1212 | 甲代烯丙基 | H | i-Pr | H | H | H | H | Ph |
1213 | 甲代烯丙基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1214 | 甲代烯丙基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1215 | 甲代烯丙基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1216 | 甲代烯丙基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1217 | 甲代烯丙基 | H | i-Bu | H | H | H | H | Ph |
1218 | 甲代烯丙基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1219 | 甲代烯丙基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1220 | 甲代烯丙基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1221 | 甲代烯丙基 | H | i-Bu | H | H | H | H | 2-Naph |
表1-35
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1222 | 1,2-二甲基丙基 | H | Me | H | H | H | H | Ph |
1223 | 1,2-二甲基丙基 | H | Me | H | H | H | H | 4-ClC6H4 |
1224 | 1,2-二甲基丙基 | H | Me | H | H | H | H | 4-MeC6H4 |
1225 | 1,2-二甲基丙基 | H | Me | H | H | H | H | 噻吩-2-基 |
1226 | 1,2-二甲基丙基 | H | Me | H | H | H | H | 吡啶-2-基 |
1227 | 1,2-二甲基丙基 | H | i-Pr | H | H | H | H | Ph |
1228 | 1,2-二甲基丙基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1229 | 1,2-二甲基丙基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1230 | 1,2-二甲基丙基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1231 | 1,2-二甲基丙基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1232 | 1,2-二甲基丙基 | H | i-Bu | H | H | H | H | Ph |
1233 | 1,2-二甲基丙基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1234 | 1,2-二甲基丙基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1235 | 1,2-二甲基丙基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1236 | 1,2-二甲基丙基 | H | i-Bu | H | H | H | H | 1-Naph |
1237 | 4-MeOC6H4CH2 | H | Me | H | H | H | H | Ph |
1238 | 4-MeOC6H4CH2 | H | Me | H | H | H | H | 4-ClC6H4 |
1239 | 4-MeOC6H4CH2 | H | Me | H | H | H | H | 4-MeC6H4 |
1240 | 4-MeOC6H4CH2 | H | Me | H | H | H | H | 呋喃-2-基 |
1241 | 4-MeOC6H4CH2 | H | Me | H | H | H | H | 吡啶-4-基 |
1242 | 4-MeOC6H4CH2 | H | i-Pr | H | H | H | H | Ph |
1243 | 4-MeOC6H4CH2 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1244 | 4-MeOC6H4CH2 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1245 | 4-MeOC6H4CH2 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1246 | 4-MeOC6H4CH2 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1247 | 4-MeQC6H4CH2 | H | i-Bu | H | H | H | H | Ph |
1248 | 4-MeOC6H4CH2 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1249 | 4-MeOC6H4CH2 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1250 | 4-MeOC6H4CH2 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1251 | 4-MeOC6H4CH2 | H | i-Bu | H | H | H | H | 2-Naph |
表1-36
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1252 | 2-甲硫基乙基 | H | Me | H | H | H | H | Ph |
1253 | 2-甲硫基乙基 | H | Me | H | H | H | H | 4-ClC6H4 |
1254 | 2-甲硫基乙基 | H | Me | H | H | H | H | 4-MeC6H4 |
1255 | 2-甲硫基乙基 | H | Me | H | H | H | H | 噻吩-2-基 |
1256 | 2-甲硫基乙基 | H | Me | H | H | H | H | 吡啶-2-基 |
1257 | 2-甲硫基乙基 | H | i-Pr | H | H | H | H | Ph |
1258 | 2-甲硫基乙基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1259 | 2-甲硫基乙基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1260 | 2-甲硫基乙基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1261 | 2-甲硫基乙基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1262 | 2-甲硫基乙基 | H | i-Bu | H | H | H | H | Ph |
1263 | 2-甲硫基乙基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1264 | 2-甲硫基乙基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1265 | 2-甲硫基乙基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1266 | 2-甲硫基乙基 | H | i-Bu | H | H | H | H | 1-Naph |
1267 | 2-甲磺酰基乙基 | H | Me | H | H | H | H | Ph |
1268 | 2-甲磺酰基乙基 | H | Me | H | H | H | H | 4-ClC6H4 |
1269 | 2-甲磺酰基乙基 | H | Me | H | H | H | H | 4-MeC6H4 |
1270 | 2-甲磺酰基乙基 | H | Me | H | H | H | H | 呋喃-2-基 |
1271 | 2-甲磺酰基乙基 | H | Me | H | H | H | H | 吡啶-4-基 |
1272 | 2-甲磺酰基乙基 | H | i-Pr | H | H | H | H | Ph |
1273 | 2-甲磺酰基乙基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1274 | 2-甲磺酰基乙基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1275 | 2-甲磺酰基乙基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1276 | 2-甲磺酰基乙基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1277 | 2-甲磺酰基乙基 | H | i-Bu | H | H | H | H | Ph |
1278 | 2-甲磺酰基乙基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1279 | 2-甲磺酰基乙基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1280 | 2-甲磺酰基乙基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1281 | 2-甲磺酰基乙基 | H | i-Bu | H | H | H | H | 2-Naph |
表1-37
化合物序号 | R17 | R18 | R19 | R20 | R21 | R22 | R23 | R24 |
1282 | 2-噻吩基 | H | Me | H | H | H | H | Ph |
1283 | 2-噻吩基 | H | Me | H | H | H | H | 4-ClC6H4 |
1284 | 2-噻吩基 | H | Me | H | H | H | H | 4-MeC6H4 |
1285 | 2-噻吩基 | H | Me | H | H | H | H | 噻吩-2-基 |
1286 | 2-噻吩基 | H | Me | H | H | H | H | 吡啶-2-基 |
1287 | 2-噻吩基 | H | i-Pr | H | H | H | H | Ph |
1288 | 2-噻吩基 | H | i-Pr | H | H | H | H | 4-ClC6H4 |
1289 | 2-噻吩基 | H | i-Pr | H | H | H | H | 3,4-Cl2C6H3 |
1290 | 2-噻吩基 | H | i-Pr | H | H | H | H | 2-MeC6H4 |
1291 | 2-噻吩基 | H | i-Pr | H | H | H | H | 4-MeC6H4 |
1292 | 2-噻吩基 | H | i-Bu | H | H | H | H | Ph |
1293 | 2-噻吩基 | H | i-Bu | H | H | H | H | 2-ClC6H4 |
1294 | 2-噻吩基 | H | i-Bu | H | H | H | H | 3-ClC6H4 |
1295 | 2-噻吩基 | H | i-Bu | H | H | H | H | 4-ClC6H4 |
1296 | 2-噻吩基 | H | i-Bu | H | H | H | H | 1-Naph |
表2-1:分析数据
化合物序列 | 分析数据 |
4 | 1H NMR(CDCl3,ppm);1.15(3H,d,J=6.1Hz),3.46-3.61(2H,m),3.63(3H,s),3.66-3.72(1H,m),4.86(1H,d,J=8.5Hz),6.86(1H,br-s),7.41(2H,d,J=8.1Hz),7.74(2H,d,J=8.1Hz). |
26 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=8.1Hz),1.85-1.89(1H,m),3.46-3.61(2H,m),3.63(3H,s),3.66-3.72(1H,m),4.86(1H,d,J=8.5Hz),6.86(1H,br-s),7.39-7.49(3H,m),7.79(2H,d,J=7.1Hz). |
30 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=8.1Hz),1.85-1.89(1H,m),2.39(3H,s),3.46-3.61(2H,m),3.63(3H,s),3.66-3.72(1H,m),4.86(1H,d,J=8.5Hz),6.86(1H,br-s),7.23(2H,d,J=8.1Hz),7.68(2H,d,J=8.1Hz). |
66 | 1H NMR(CDCl3,ppm):3.46-3.61(2H,m),3.63(3H,s),3.66-3.72(1H,m),4.86(1H,d,J=8.5Hz),6.86(1H,br-s),7.23-7.41(6H,m),7.39-7.49(3H,m),7.791(2H,d,J=7.1Hz). |
215 | 1H NMR(CDCl3,ppm):1.14(3H,d,J=6.1Hz),1.22(3H,d,J=6.8Hz),1.24(3H,d,J=6.8Hz),2.39(3H,s),3.48-3.53(2H,m),3.96-3.99(1H,m),4.79(1H,br-s),4.84-4.91(1H,m),7.23(2H,d,J=8.1Hz),7.70(2H,d,J=8.1Hz). |
216 | 1H NMR(CDCl3,ppm):1.14(3H,d,J=6.1Hz),1.22(3H,d,J=6.8Hz),1.24(3H,d,J=6.8Hz),1.32(9H,s),3.48-3.53(2H,m),3.96-3.99(1H,m),4.79(1H,br-s),4.84-4.91(1H,m),7.23(2H,d,J=8.1Hz),7.70(2H,d,J=8.1Hz). |
236 | 1H NMR(CDCl3,ppm):1.01(6H,t,J=7.1Hz),1.09(3H,d,J=6.1Hz),1.22(3H,d,J=6.1Hz),1.85-1.89(1H,m),3.48-3.61(2H,m),3.68-3.74(1H,m),4.12(1H,d,J=7.3Hz),4.73-4.89(1H,m),7.06(1H,br-s),7.40-7.50(3H,m),7.80(2H,d,J=7.1Hz). |
237 | 1H NMR(CDCl3,ppm):1.00(3H,d,J=6.8Hz),1.01(3H,d,J=6.8Hz),1.11(3H,d,J=6.1Hz),1.23(3H,d,J=6.1Hz),1.85-1.90(1H,m),3.50-3.54(2H,m),3.67-3.73(1H,m),4.73(1H,d,J=8.8Hz),4.83-4.90(1H,m),7.21(1H,br-s),7.40(2H,d,J=8.5Hz),7.75(2H,d,J=8.5Hz). |
238 | 1H NMR(CDCl3,ppm):1.01(6H,t,J=6.8Hz),1.14(3H,d,J=6.3Hz),1.24(3H,d,J=6.3Hz),1.85-1.90(1H,m),3.50-3.53(2H,m),3.67-3.72(1H,m),4.75(1H,d,J=8.3Hz),4.86-4.92(1H,m),7.35(1H,br-s),7.50(1H,d,J=8.3Hz),7.62(1H,d,J=8.3Hz),7.94(1H,s). |
239 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=6.8Hz),1.00(3H,d,J=6.8Hz),1.17(3H,d,J=6.3Hz),1.21(3H,d,J=6.3Hz),1.83-1.88(1H,m),2.44(3H,s),3.41-3.47(1H,m),3.56-3.70(2H,m),4.77(1H,d,J=8.5Hz),4.82-4.88(1H,m),6.29(1H br-s),7.16-7.35(4H,m). |
表2-2:分析数据
化合物序号 | 分析数据 |
240 | 1H NMR(CDCl3,ppm):0.99(3H,d,J=7.3Hz),1.01(3H,d,J=7.3Hz),1.10(3H,d,J=6.1Hz),1.21(3H,d,J=6.1Hz),1.84-1.88(1H,m),2.38(3H,s),3.47-3.60(2H,m),3.67-3.73(1H,m),4.75(1H,d,J=8.5Hz),4.83-4.89(1H,m),6.99(1H,br-s),7.22(2H,d,J=8.1Hz),7.69(2H,d,J=8.1Hz). |
241 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.3Hz),1.09(3H,d,J=6.2Hz),1.21-1.26(6H,m),1.82-1.90(1H,m),2.68(2H,q,J=7.6Hz),3.46-3.62(2H,m),3.68-3.76(1H,m),4.74(1H,d,J=8.8Hz),4.87-4.90(1H,m),6.99(1H,d,J=8.1Hz),7.24(2H,d,J=8.5Hz),7.72(2H,d,J=8.5Hz). |
242 | 1H NMR(CDCl3,ppm):1.03(6H,t,J=6.8Hz),1.09(3H,d,J=6.1Hz),1.22(3H,d,J=6.1Hz),1.87-1.92(1H,m),3.54-3.67(2H,m),3.74-3.78(1H,m),4.77(1H,d,J=8.5Hz),4.86-4.92(1H,m),7.23(1H,br-s),7.51-7.58(2H,m),7.86-7.94(4H,m),8.34(1H,s). |
243 | 1H NMR(CDCl3,ppm):0.97-1.00(6H,m),1.11(3H,d,J=6.3Hz),1.22(3H,d,J=6.3Hz),1.80-1.90(1H,m),2.50(3H,s),3.44-3.57(2H,m),3.66-3.73(1H,m),4.76(1H,d,J=8.5Hz),4.87-4.90(1H,m),6.71(1H,d,J=3.7Hz),6.87(1H,br-s),7.30(1H,d,J=3.7Hz) |
245 | 1H NMR(CDCl3,ppm):0.93(3H,d,J=7.1Hz),0.95(3H,d,J=7.1Hz),1.15(3H,s),1.23(6H,d,J=6.3Hz),2.35-2.40(4H,m),3.60(1H,dd,J=5.1Hz,14.2Hz),3.82(1H,dd,J=5.9Hz,14.2Hz),4.72(1H,br-s),4.87-4.93(1H,m),7.24(2H,d,J=8.1Hz),7.76(2H,d,J=8.1Hz). |
246 | 1H NMR(CDCl3,ppm):1.00-1.03(6H,m),1.17(3H,d,J=6.6Hz),1.26(6H,d,J=6.3Hz),1.65-1.69(1H,m),2.39(3H,s),3.51-3.56(1H,m),4.33-4.37(1H,m),4.56(1H,d,J=8.0Hz),4.92-5.00(1H,m),7.23(2H,d,J=8.3Hz),7.30(1H,br-s),7.72(2H,d,J=8.3Hz). |
247 | 1H NMR(CDCl3,ppm):0.99-1.03(6H,m),1.18(3H,d,J=6.6Hz),1.26(6H,d,J=6.3Hz),1.62-1.67(1H,m),3.50-3.54(1H,m),4.33-4.35(1H,m),4.53(1H,d,J=8.0Hz),4.91-4.98(1H,m),7.22(2H,d,J=8.3Hz),7.31(1H,br-s),7.74(2H,d,J=8.3Hz). |
279 | 1H NMR(CDCl3,ppm):1.15-1.26(6H,m),2.40(3H,s),3.25-3.30(1H,m),3.42-3.50(1H,m),4.82-4.90(1H,m),4.92-4.98(1H,m),5.60(1H,d,J=7.1Hz),6.84(1H,br-s),7.22-7.40(7H,m),7.67(2H,d,J=7.8Hz). |
284 | 1H NMR(CDCl3,ppm):1.13-1.19(6H,m),2.40(3H,m),3.70-3.80(2H,m),4.82-4.92(2H,m),5.80(1H,d,J=7.1Hz),6.65(1H,br-s),7.21-7.29(4H,m),7.34(2H,d,J=8.1Hz),7.65(2H,d,J=8.1Hz).M+:375. |
表2-3:分析数据
化合物序号 | 分析数据 |
289 | 1H NMR(CDCl3,ppm):1.12(3H,d,J=6.1Hz),1.18(3H,d,J=6.1Hz),2.38(3H,s),2.80-2.86(1H,m),2.92-2.98(1H,m),3.49-3.56(2H,m),4.07-4.15(1H,m),4.81-4.88(1H,m),4.95(1H,d,J=7.3Hz),6.88(1H,br-s),7.20-7.27(5H,m),7.31(2H,d,J=8.1Hz),7.65(2H,d,J=8.1Hz). |
290 | 1H NMR(CDCl3,ppm):1.12(3H,d,J=6.1Hz),1.18(3H,d,J=6.1Hz),1.20-1.25(3H,m),2.67(2H,q,J=7.6Hz),2.80-2.86(1H,m),2.92-2.98(1H,m),3.49-3.56(2H,m),4.07-4.15(1H,m),4.81-4.88(1H,m),4.95(1H,d,J=7.3Hz),6.88(1H,br-s),7.20-7.27(5H,m),7.31(2H,d,J=8.1Hz),7.65(2H,d,J=8.1Hz). |
384 | 1H NMR(CDCl3,ppm),0.85(3H,d,J=6.6Hz),0.86(3H,d,J=6.6Hz),1.01(6H,t,J=6.6Hz),1.79-1.89(1H,m),3.47-3.71(3H,m),3.80(2H,d,J=6.8Hz),4.82(1H,d,J=8.3Hz),6.92(br-s),7.41(2H,d,J=8.3Hz),7.76(2H,d,J=8.3Hz). |
387 | 1H NMR(CDCl3,ppm):0.84(3H,d,J=6.8Hz),0.85(3H,d,J=6.8Hz),1.06(6H,d,J=6.8Hz),1.63-1.89(2H,m),2.39(3H,s),3.46-3.74(3H,m),3.80(2H,d,J=6.6Hz),4.82(1H,d,J=8.8Hz),6.92(1H,br-s),7.22(2H,d,J=7.8Hz),7.68(2H,d,J=7.8Hz). |
464 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=6.8Hz),1.39(9H,s),1.82-1.87(1H,m),2.38(3H,s),3.46-3.53(2H,m),3.65-3.69(1H,m),4.65(1H,d,J=8.5Hz),7.04(1H,br-s),7.21(2H,d,J=8.1Hz),7.70(2H,d,J=8.1Hz). |
469 | 1H NMR(CDCl3,ppm):0.92(3H,d,J=6.8Hz),0.94(3H,d,J=6.8Hz),1.13(3H,s),2.37-2.41(4H,m),3.57(1H,dd,J=5.6hz),13.7Hz),3.81(1H,dd,J=5.6Hz),13.7Hz),4.62(1H,br-s),7.24(2H,d,J=8.1Hz),7.77(2H,d,J=8.1Hz),8.17(1H,br-s). |
470 | 1H NMR(CDCl3,ppm):1.00-1.03(6H,m),1.17(3H,d,J=6.6Hz),1.49(9H,s),1.58-1.67(1H,m),3.47-3.53(1H,m),4.33-4.35(1H,m),4.51(1H,d,J=8.0Hz),7.23(2H,d,J=8.3Hz),7.38(1H,br-s),7.73(2H,d,J=8.3Hz). |
471 | 1H NMR(CDCl3,ppm):1.00-1.03(6H,m),1.16(3H,d,J=6.6Hz),1.49(9H,s),1.59-1.68(1H,m),2.38(3H,s),3.46-3.52(1H,m),4.33-4.35(1H,m),4.51(1H,d,J=8.0Hz),7.21(2H,d,J=8.3Hz),7.36(1H,br-s),7.72(2H,d,J=8.3Hz). |
504 | 1H NMR(CDCl3,ppm):1.40(9H,s),2.40(3H,s),3.25-3.30(1H,m),3.42-3.50(1H,m),4.82-4.90(1H,m),5.60(1H,d,J=7.1Hz),6.84(1H,br-s),7.22-7.40(7H,m),7.67(2H,d,J=7.8Hz). |
表2-4:分析数据
化合物序号 | 分析数据 |
526 | 1H NMR(CDCl3,ppm):1.05(3H,d,J=6.8Hz),1.07(3H,d,J=6.8Hz),1.91-1.96(1H,m),2.40(3H,s),3.47-3.50(1H,m),3.74-3.78(2H,m),5.26(1H,d,J=7.6Hz),6.76(1H,br-s),7.15-7.31(5H,m),7.40-7.50(3H,m),7.80(2H,d,J=7.3Hz). |
530 | 1H NMR(CDCl3,ppm):1.05(3H,d,J=6.8Hz),1.07(3H,d,J=6.8Hz),1.91-1.96(1H,m),2.40(3H,s),3.47-3.50(1H,m),3.74-3.78(2H,m),5.26(1H,d,J=7.6Hz),6.76(1H,br-s),6.95(2H,d,J=8.3Hz),7.15-7.31(5H,m),7.68(2H,d,J=8.3Hz). |
596 | 1H NMR(CDCl3,ppm):0.99(3H,d,J=6.8Hz),1.01(3H,d,J=6.8Hz),1.85-1.90(1H,m),2.39(3H,s),3.48-3.62(2H,m),3.69-3.74(1H,m),4.94(1H,d,J=8.8Hz),5.06(2H,d,J=7.1Hz),6.85(1H,br-s),7.20-7.30(7H,m),7.41-7.51(3H,m),7.79(2H,d,J=7.1Hz). |
600 | 1H NMR(CDCl3,ppm):0.99(3H,d,J=6.8Hz),1.01(3H,d,J=6.8Hz),1.85-1.90(1H,m),2.39(3H,s),3.48-3.62(2H,m),3.69-3.74(1H,m),4.94(1H,d,J=8.8Hz),5.06(2H,d,J=7.1Hz),6.86(1H,br-s),7.20-7.30(7H,m),7.65(2H,d,J=8.1Hz). |
636 | 1H NMR(CDCl3,ppm):3.48-3.62(2H,m),3.69-3.74(1H,m),4.94(1H,d,J=8.8Hz),5.06(2H,d,J=7.1Hz),6.86(1H,br-s),7.20-7.40(14H,m),7.82(2H,d,J=7.1Hz). |
874 | 1H NMR(CDCl3,ppm):1.10(3H,d,J=6.8Hz),1.12(3H,d,J=6.8Hz),1.94-2.01(1H,m),3.50-3.55(1H,m),3.80-3.84(2H,m),5.31(1H,d,J=8.5Hz),6.78(1H,br-s),7.10(1H,d,J=8.8Hz),7.21(2H,d,J=7.8Hz),7.37(1H,s),7.41-7.56(2H,m),7.60-7.90(5H,m), |
677 | 1H NMR(CDCl3,ppm):1.09(3H,d,J=6.8Hz),1.10(3H,d,J=6.8Hz),1.94-1.99(1H,m),2.40(3H,s),3.47-3.51(1H,m),3.80-3.84(2H,m),5.30(1H,d,J=8.5Hz),6.77(1H,br-s),7.10(1H,d,J=8.8Hz),7.21(2H,d,J=7.8Hz),7.34(1H,s),7.41-7.54(2H,m),7.63-7.93(5H,m). |
739 | 1H NMR (CDCl3,ppm):1.00(6H,t,J=7.3Hz),1.85-1.90(1H,m),3.46-3.74(3H,m),4.52(2H,d,J=5.6Hz),4.93(1H,d,J=8.3Hz),5.14(1H,d,J=10.5Hz),5.25(1H,d,J=17.1Hz),4.79-5.88(1H,m),6.88(1H,br-s),7.39(2H,d,J=8.1Hz),7.73(2H,d,J=8.1Hz). |
742 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.3Hz),1.85-1.90(1H,m),2.39(3H,s),3.46-3.74(3H,m),4.52(2H,d,J=5.6Hz),4.93(1H,d,J=8.3Hz),5.14(1H,d,J=10.5Hz),5.25(1H,d,J=17.1Hz),4.79-5.88(1H,m),6.88(1H,br-s),7.22(2H,d,J=8.1Hz),7.68(2H,d,J=8.1Hz). |
表2-5:分析数据
化合物序号 | 分析数据 |
804 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.8Hz),1.86-1.91(1H,m),2.36(1H,s),3.47-3.74(3H,m),4.63(2H,s),5.01(1H,d,J=9.0Hz),6.79(1H,br-s),7.38(2H,d,J=8.1Hz),7.73(2H,d,J=8.1Hz). |
807 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.8Hz),1.86-1.91(1H,m),2.36(1H,s),2.39(3H,s),3.47-3.74(3H,m),4.63(2H,s),5.01(1H,d,J=9.0Hz),6.79(1H,br-s),7.22(2H,d,J=8.1Hz),7.68(2H,d,J=8.1Hz). |
1049 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=7.1Hz),1.00(3H,d,J=7.1Hz),1.84-1.89(1H,m),2.31(3H,s),3.49-3.57(2H,m),3.69-3.75(1H,m),4.92(1H,d,J=9.0Hz),5.00(1H,d,J=12.2Hz),5.05(1H,d,J=12.2Hz),7.00(1H,br-s),7.07(2H,d,J=8.1Hz),7.16(2H,d,J=7.8Hz),7.24(2H,d,J=8.1Hz),7.67(2H,d,J=7.8Hz). |
1050 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=7.1Hz),1.00(3H,d,J=7.1Hz),1.84-1.89(1H,m),2.31(3H,s),2.40(3H,s),3.49-3.57(2H,m),3.69-3.75(1H,m),4.92(1H,d,J=9.0Hz),5.00(1H,d,J=12.2Hz),5.05(1H,d,J=12.2Hz),7.00(1H,br-s),7.07(2H,d,J=8.1Hz),7.16(2H,d,J=7.8Hz),7.22(2H,d,J=8.1Hz),7.65(2H,d,J=7.8Hz). |
1063 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.1Hz),1.83-1.90(1H,m),3.43-3.47(1H,m),3.62-3.73(2H,m),4.94(1H,d,J=12.4Hz),4.95(1H,d,J=9.0Hz),5.06(1H,d,J=12.4Hz),6.73(1H,br-s),7.17-7.22(6H,m),7.59(2H,d,J=8.1Hz). |
1066 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.1Hz),1.83-1.90(1H,m),2.41(3H,s),3.43-3.47(1H,m),3.62-3.73(2H,m),4.94(1H,d,J=12.4Hz),4.95(1H,d,J=9.0Hz),5.06(1H,d,J=12.4Hz),6.73(1H,br-s),7.17-7.22(6H,m),7.61(2H,d,J=8.1Hz). |
1078 | 1H NMR(CDCl3,ppm):0.95-1.02(6H,m),1.39(3×1/2H,d,J=6.6Hz),1.51(3H×1/2,d,J=6.6Hz),1.80-1.88(1H,m),3.40-3.64(3H,m),4.90(1H×1/2,d,J=8.5Hz),4.96(1H×1/2,d,J=9.0Hz),5.70-5.77(1H,m),6.71(1H×1/2,br-s),6.78(1H×1/2,br-s),7.09-7.36(6H,m),7.45(2H×1/2,d,J=8.3Hz),7.69(2H×1/2,d,J=8.3Hz). |
1081 | 1H NMR(CDCl3,ppm):0.95-1.02(6H,m),1.39(3H×1/2,d,J=6.6Hz),1.51(3H×1/2,d,J=6.6Hz),1.80-1.88(1H,m),2.37(3H×1/2,s),2.40(3H×1/2,s),3.40-3.64(3H,m),4.90(1H×1/2,d,J=8.5Hz),4.96(1H×1/2,d,J=9.0Hz),5.70-5.77(1H,m),6.71(1H×1/2,br-s),6.78(1H×1/2,br-s),7.09-7.36(6H,m),7.47(2H×1/2,d,J=8.3Hz),7.71(2H×1/2,d,J=8.3Hz). |
表2-6:分析数据
化合物序号 | 分析数据 |
1123 | 1H NMR(CDCl3,ppm):0.99(3H,d,J=6.8Hz),1.02(3H,d,J=6.8Hz),1.85-1.89(1H,m),3.51-3.54(2H,m),3.72-3.76(1H,m),4.90(1H,d,J=9.0Hz),5.02(2H,d,J=4.9Hz),6.29(1H,d,J=3.2Hz),6.31(1H,d,J=3.2Hz),6.85(1H,br-s),7.20(2H,d,J=8.1Hz),7.33(1H,s),7.66(2H,d,J=8.1Hz). |
1126 | 1H NMR(CDCl3,ppm):0.88(3H,d,J=6.8Hz),1.00(3H,d,J=6.8Hz),1.85-1.89(1H,m),2.40(3H,s),3.51-3.54(2H,m),3.70-3.76(1H,m),4.90(1H,d,J=9.0Hz),5.02(2H,d,J=4.9Hz),6.29(1H,d,J=3.2Hz),6.33(1H,d,J=3.2Hz),6.87(1H,br-s),7.23(2H,d,J=8.1Hz),7.33(1H,s),7.68(2H,d,J=8.1Hz). |
1138 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=6.8Hz),1.00(3H,d,J=6.8Hz),1.84-1.89(1H,m),3.48-3.61(2H,m),3.68-3.73(1H,m),4.88(1H,d,J=6.8Hz),4.92(2H,s),6.34(1H,s),6.80(1H,br-s),7.20(2H,d,J=7.8Hz),7.29(1H,d,J=2.0Hz),7.41(1H,d,J=2.0Hz),7.63(2H,d,J=7.8Hz). |
1141 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=6.8Hz),1.00(3H,d,J=6.8Hz),1.84-1.89(1H,m),2.40(3H,s),3.48-3.61(2H,m),3.68-3.73(1H,m),4.88(1H,d,J=6.8Hz),4.92(2H,s),6.33(1H,s),6.83(1H,br-s),7.22(2H,d,J=7.8Hz),7.31(1H,d,J=2.0Hz),7.39(1H,d,J=2.0Hz),7.65(2H,d,J=7.8Hz). |
1153 | 1H NM(CDCl3,ppm):1.00(3H,d,J=6.8Hz),1.01(3H,d,J=6.8Hz),1.49-1.56(1H,m),1.81-1.95(4H,m),3.51-3.54(2H,m),3.65-4.16(6H,m),4.95(1H,d,J=8.5Hz),6.91(1H,br-s),7.24(2H,d,J=8.1Hz),7.70(2H,d,J=8.1Hz). |
1156 | 1H NMR(CDCl3,ppm):0.99(3H,d,J=6.8Hz),1.01(3H,d,J=6.8Hz),1.49-1.56(1H,m),1.81-1.95(4H,m),2.39(3H,s),3.51-3.55(2H,m),3.67-4.16(6H,m),4.95(1H,d,J=8.5Hz),6.93(1H,br-s),7.22(2H,d,J=8.1Hz),7.68(2H,d,J=8.1Hz). |
1168 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=6.8Hz),1.00(3H,d,J=6.8Hz,1.85-1.89(1H,m),3.51-3.56(2H,m),3.70-3.75(1H,m),4.91(1H,d,J=8.8Hz),5.19(1H,d,J=12.7Hz),5.22(1H,d,J=12.7Hz),6.83(1H,br-s),6.91(1H,dd,J=1.7Hz,3.4Hz),7.01(1H,dd,J=1.7Hz,3.4Hz),7.21-7.25(3H,m),7.68(2H,d,J=8.1Hz). |
表2-7:分析数据
化合物序号 | 分析数据 |
1171 | 1H NMR(CDCl3,ppm):0.98(3H,d,J=6.8Hz),1.00(3H,d,J=6.8Hz),1.85-1.89(1H,m),2.40(3H,s),3.51-3.56(2H,m),3.70-3.75(1H,m),4.92(1H,d,J=8.8Hz),5.19(1H,d,J=12.7Hz),5.22(1H,d,J=12.7Hz),6.85(1H,br-s),6.91(1H,dd,J=1.7Hz,3.4Hz),7.01(1H,dd,J=1.7Hz,3.4Hz),7.21-7.24(3H,m),7.66(2H,d,J=8.1Hz). |
1183 | 1H NMR(CDCl3,ppm):0.19-0.23(2H,m),0.45-0.50(2H,m),1.01(6H,t,J=7.1Hz),1.86-1.93(1H,m),3.48-3.64(2H,m),3.67-3.75(1H,m),3.85(2H,d,J=7.3Hz),4.87(1H,d,J=9.0Hz),6.98(1H,br-s),7.23(2H,d,J=8.5Hz),7.69(2H,d,J=8.5Hz). |
1186 | 1H NMR(CDCl3,ppm):0.19-0.23(2H,m),0.45-0.49(2H,m),1.01(6H,t,J=7.1Hz),1.86-1.93(1H,m),2.38(3H,s),3.48-3.62(2H,m),3.67-3.75(1H,m),3.84(2H,d,J=7.3Hz),4.86(1H,d,J=9.0Hz),6.98(1H,br-s),7.21(2H,d,J=8.5Hz),7.68(2H,d,J=8.5Hz). |
1198 | 1H NMR(CDCl3,ppm):0.88(9H,s),1.03(6H,t,J=5.6Hz),1.86-1.90(1H,m),3.48-3.68(2H,m),3.70-3.75(3H,m),4.84(1H,d,J=8.5Hz),6.92(1H,d,J=6.6Hz),7.20(2H,d,J=8.1Hz),7.65(2H,d,J=8.1Hz). |
1201 | 1H NMR(CDCl3,ppm):0.86(9H,s),1.01(6H,t,J=5.6Hz),1.86-1.91(1H,m),2.39(3H,s),3.48-3.68(2H,m),3.70-3.76(3H,m),4.84(1H,d,J=8.5Hz),6.94(1H,d,J=6.6Hz),7.22(2H,d,J=8.1Hz),7.67(2H,d,J=8.1Hz). |
1213 | 1H NMR(CDCl3,ppm):1.03(6H,t,J=7.1Hz),1.68(3H,s),1.84-1.90(1H,m),3.48-3.75(3H,m),4.45(2H,s),4.83(1H,s),4.90-4.95(2H,m),6.87(1H,br-s),7.22(2H,d,J=8.1Hz),7.68(2H,d,J=8.1Hz). |
1216 | 1H NMR(CDCl3,ppm),1.01(6H,t,J=7.1Hz),1.67(3H,s),1.84-1.90(1H,m),2.39(3H,s),3.46-3.75(3H,m),4.44(2H,s),4.83(1H,s),4.90-4.94(2H,m),6.87(1H,br-s),7.21(2H,d,J=8.1Hz),7.67(2H,d,J=8.1Hz). |
1228 | 1H NMR(CDCl3,ppm):0.75(3H,d,J=6.6Hz),0.90(3H,d,J=6.6Hz),1.01(6H+3H×1/2,t,J=6.6Hz),1.13(3H×1/2,d,J=6.6Hz),1.82-1.91(1H,m),3.45-3.65(2H,m),3.69-3.77(1H,m),4.56-4.61(1H,m),4.75(1H,t,J=8.1Hz),6.94(1H,d,J=9.0Hz),7.20-7.24(2H,m),7.66(2H,t,J=7.6Hz). |
表2-8:分析数据
化合物序号 | 分析数据 |
1231 | 1H NMR(CDCl3,ppm):0.75(3H,d,J=6.6Hz),0.89(3H,d,J=8.6Hz),1.01(6H+3H×1/2,t,J=6.6Hz),1.14(3H×1/2,d,J=6.6Hz),1.82-1.91(1H,m),2.38(3H,s),3.45-3.65(2H,m),3.69-3.76(1H,m),4.56-4.62(1H,m),4.75(1H,t,J=8.1Hz),6.95(1H,d,J=9.0Hz),7.20-7.23(2H,m),7.68(2H,t,J=7.6Hz). |
1258 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.6Hz),1.86-1.92(1H,m),2.05(3H,s),2.62(2H,t,J=6.8Hz),3.47-3.73(3H,m),4.15-4.24(2H,m),4.89(1H,d,J=8.5Hz),6.84(1H,br-s),7.22(2H,d,J=8.1Hz),7.67(2H,d,J=8.1Hz). |
1261 | 1H NMR(CDCl3,ppm):1.00(6H,t,J=7.6Hz),1.86-1.91(1H,m),2.07(3H,s),2.39(3H,s),2.62(2H,t,J=6.8Hz),3.47-3.72(3H,m),4.15-4.23(2H,m),4.89(1H,d,J=8.5Hz),6.81(1H,br-s),7.23(2H,d,J=8.1Hz),7.68(2H,d,J=8.1Hz). |
1273 | 1H NMR (CDCl3,ppm):0.98(3H,d,J=6.8Hz),1.02(3H,d,J=6.8Hz),1.83-1.90(1H,m),2.40(3H,s),3.13-3.18(2H,m),3.41-3.45(1H,m),3.66-3.70(2H,m),4.34-4.40(1H,m),4.49-4.54(1H,m),5.20(1H,d,J=8.1Hz),6.64(1H,br-s),7.26(2H,d,J=7.8Hz),7.65(2H,d,J=7.8Hz). |
1276 | 1H NMR(CDCl3,ppm):0.99(3H,d,J=6.8Hz),1.01(3H,d,J=6.8Hz),1.83-1.90(1H,m),2.40(3H,s),2.81(3H,s),3.13-3.16(2H,m),3.41-3.45(1H,m),3.66-3.70(2H,m),4.34-4.40(1H,m),4.49-4.55(1H,m),5.19(1H,d,J=8.1Hz),6.66(1h,br-s),7.24(2H,d,J=7.8Hz),7.66(2H,d,J=7.8Hz). |
配方的实施例及试验例
以下说明本发明杀菌剂的配方的实施例及活性试验。在以下实施例中,“份数”是指“重量份数”或“重量%”。
配方实施例1:颗粒
将30份的本发明化合物(30),22份斑脱土,45份滑石,3份Sorpol5060(表面活性剂:Toho Chemical Industry Co.,Ltd.,商品名称)与少量防沫剂均匀捏合,使用篮式制粒机进行制粒,干燥后得到100份颗粒。
配方实施例2:颗粒
将15份本发明化合物(241),60份斑脱土,21份滑石,1份十二烷基苯磺酸钠,1份聚氧乙烯烷基烯丙基醚与2份木质素磺酸钠进行混合,加入适量的水均匀捏合,使用篮式制粒机进行制粒,干燥后得到100份颗粒。
配方实施例3:可湿性粉末
将50份本发明化合物(290),40份碳酸钙,5份Sorpol 5039(阴离子表面活性剂与白炭墨(二氧化硅)的混合物:Toho Chemical IndustryCo.,Ltd.,商品名称)与5份白炭墨混合,并均匀研磨得到可湿性粉末。
配方实施例4:可湿性粉末
将30份本发明化合物(526),63份高岭石,5份Sorpol 5039(阴离子表面活性剂与白炭墨的混合物:Toho Chemical Industry Co.,Ltd.,商品名称)与2份白炭墨混合,并均匀研磨得到可湿性粉末。
配方实施例5:乳液
将20份本发明化合物(674),55份二甲苯,20份N,N-二甲基甲酰胺与5份Sorpol 2680(表面活性剂)均匀混合,得到乳化浓缩物。
配方实施例6:易流动物质
在由40份本发明化合物(742)、5份Sorpol 3353(非离子表面活性剂:Toho Chemical Industry Co.,Ltd.,商品名称)、5份1%黄原胶水溶液,40份水和10份乙二醇构成的所有组份中,除了活性成分外,使其他的组份都进行均匀地溶解,然后加入本发明化合物。充分搅拌后,使用砂磨机进行湿研磨,得到可流动物质。
配方实施例7:粉末
将5份本发明化合物(807)与95份粘土混合得到粉末。
试验例1:稻瘟病控制效果试验(喷雾应用试验)
将按照配方实施例4制备的可湿性粉末配置成的500ppm稀释溶液施于水稻罐(rice pot)(品种:Koshihikari;两叶期),并空气干燥。该植物被置于人工气候室(设定条件:22℃,12小时黑暗和光明循环)并被喷雾接种稻瘟病菌(Pyricularia oryzae)孢子悬浮液。人工气候室保持高湿度,植物在7天后接受检查。按照下面的方程式计算预期值,并在下表中所列出的标准的基础上评价控制效果。结果如表3所示。
预期值(%)=(1-处理过的小块土地中的损伤数目/未处理过的小块土地中的损伤数目)×100
效果 | 预期值 |
A | 100% |
B | 80%或更多,但小于100% |
C | 50%或更多,但小于80% |
D | 小于50% |
作为对照,使用如下化学物质。
结构式(7):
结构式(8):
表3-1:稻瘟病控制效果试验(喷雾应用试验)
化合物序号 | 效果等级 |
4 | A |
26 | A |
30 | A |
66 | A |
215 | A |
216 | A |
236 | A |
237 | A |
238 | A |
239 | A |
240 | A |
241 | A |
242 | A |
243 | A |
245 | A |
246 | A |
247 | A |
279 | A |
284 | A |
289 | A |
290 | A |
384 | A |
387 | A |
464 | B |
469 | B |
470 | A |
471 | A |
504 | B |
526 | A |
530 | A |
596 | A |
600 | A |
636 | A |
674 | A |
677 | A |
739 | A |
742 | A |
804 | A |
807 | A |
1049 | A |
1050 | A |
1063 | A |
1066 | A |
表3-2:稻瘟病控制效果试验(喷雾应用试验)
化合物序号 | 效果等级 |
1078 | A |
1081 | A |
1123 | A |
1126 | A |
1138 | A |
1141 | A |
1153 | A |
1156 | A |
1168 | A |
1171 | A |
1183 | A |
1186 | A |
1198 | A |
1201 | A |
1213 | A |
1216 | A |
1228 | A |
1231 | A |
1258 | A |
1261 | A |
1273 | A |
1276 | A |
结构式(7) | D |
结构式(8) | D |
试验例2:稻瘟病控制效果试验(水表面应用)
水稻秧苗(品种:Koshihikari;三叶期)被种植于1/5000的Wagner罐(Wagner pot)中,在温室中生长一周。将按照配方实施例2制备的颗粒以3公斤/10公亩的比率施于每个罐的水表面。施用30天后,将稻瘟病菌(Pyricularia oryzae)孢子悬浮液直接喷雾到水稻植株上。水稻植株置放于25℃和高湿度的条件下一周,检查损伤数目。按照下面的方程式计算预期值,并根据下面所列标准评价控制效果。结果如表4所示。作为对照,使用试验例1中同样的化学物质。
预期值(%)=(1-处理过的小块土地中的损伤数目/未处理过的小块土地中的损伤数目)×100
效果 | 预期值 |
A | 80%到100% |
B | 50%或更多,但小于80% |
C | 小于50% |
表4-1:稻瘟病控制效果试验(水表面应用)
化合物序号 | 效果等级 |
4 | A |
26 | A |
30 | A |
66 | A |
215 | A |
216 | A |
236 | A |
237 | A |
238 | A |
239 | A |
240 | A |
241 | A |
242 | A |
243 | A |
245 | A |
246 | A |
247 | A |
279 | A |
284 | A |
289 | A |
290 | A |
384 | A |
387 | A |
464 | B |
469 | B |
470 | A |
471 | A |
504 | B |
526 | A |
530 | A |
596 | A |
600 | A |
636 | A |
674 | A |
677 | A |
739 | A |
742 | A |
804 | A |
807 | A |
1049 | A |
1050 | A |
1063 | A |
1066 | A |
表4-2:稻瘟病控制效果试验(水表面应用)
化合物序号 | 效果等级 |
1078 | A |
1081 | A |
1123 | A |
1126 | A |
1138 | A |
1141 | A |
1153 | A |
1156 | A |
1168 | A |
1171 | A |
1183 | A |
1186 | A |
1198 | A |
1201 | A |
1213 | A |
1216 | A |
1228 | A |
1231 | A |
1258 | A |
1261 | A |
1273 | A |
1276 | A |
结构式(7) | C |
结构式(8) | C |
试验例3:稻瘟病控制效果试验(苗箱处理)
在苗箱中培育的水稻秧苗(品种:Koshihikari;两叶期)用按照配方实施例1制备的颗粒以每箱50克的量进行处理。3天后,水稻秧苗被移植到1/5000的Wagner地域中,在温室中培育。移植30天后,植株用稻瘟病菌(Pyricularia oryzae)孢子悬浮液进行喷雾接种上,并保持在25℃和高湿度条件下一周,检查损伤数目。按照下面的方程式计算预期值,并在与试验例2中同样标准的基础上评价控制效果。结果如表5所示。作为对照,使用试验例1中同样的化学物质。
预期值(%)=(1-处理过的小块土地中的损伤数目/未处理过的小块土地中的损伤数目)×100
表5-1:稻瘟病控制效果试验(苗箱处理)
化合物序号 | 效果等级 |
4 | A |
26 | A |
30 | A |
66 | A |
215 | A |
216 | A |
236 | A |
237 | A |
238 | A |
239 | A |
240 | A |
241 | A |
242 | A |
243 | A |
245 | A |
246 | A |
247 | A |
279 | A |
284 | A |
289 | A |
290 | A |
384 | A |
387 | A |
464 | B |
469 | B |
470 | A |
471 | A |
504 | B |
526 | A |
530 | A |
596 | A |
600 | A |
636 | A |
674 | A |
677 | A |
739 | A |
742 | A |
804 | A |
807 | A |
1049 | A |
1050 | A |
1063 | A |
1066 | A |
表5-2:稻瘟病控制效果试验(苗箱处理)
化合物序号 | 效果等级 |
1078 | A |
1081 | A |
1123 | A |
1126 | A |
1138 | A |
1141 | A |
1153 | A |
1156 | A |
1168 | A |
1171 | A |
1183 | A |
1186 | A |
1198 | A |
1201 | A |
1213 | A |
1216 | A |
1228 | A |
1231 | A |
1258 | A |
1261 | A |
1273 | A |
1276 | A |
结构式(7) | C |
结构式(8) | C |
工业实用性
根据本发明的二胺衍生物具有良好的控制稻瘟病的效果,但却不会伤害到有用农作物;因此,其作为一种农业和园艺用的杀菌剂是非常有效的。
Claims (15)
1.二胺衍生物,其由以下通式(1)表示:
其特征在于,
R1代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基;
R2和R7独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的芳基或酰基;
R3和R4独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基或包括结合碳原子在内的具有3到6个碳原子的的环烷基;
R5和R6独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基或可被取代的芳基;排除以下情况,即R3、R4、R5和R6都代表氢原子,或当R3、R4、R5和R6中的任何一个代表可被取代的甲基时,其他的代表氢原子;并且
R8代表可被取代的芳基或可被取代的杂芳基。
2.根据权利要求1所述的二胺衍生物,其特征在于,
R1代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基,具有2到6个碳原子的链烯基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基;
R2和R7独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基、可被取代的芳基或酰基;
R3和R4独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、可被取代的芳烷基、可被取代的杂芳烷基、可被取代的芳基或可被取代的杂芳基或包括结合碳原子在内具有3到6个碳原子的的环烷基;
R5和R6独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基或可被取代的芳基;排除以下情况,即R3、R4、R5和R6都代表氢原子,或当R3、R4、R5和R6中的任何一个代表可被取代的甲基时,其他的代表氢原子。
3.根据权利要求2所述的二胺衍生物,其特征在于,
R2和R7独立地代表氢原子、具有1到6个碳原子的烷基或酰基;
R3和R4独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基、可被取代的芳基或包括结合碳原子在内具有3到6个碳原子的的环烷基;并且
R5和R6独立地代表氢原子、具有1到6个碳原子的烷基、可被取代的芳烷基或可被取代的芳基;排除以下情况,即R3,R4,R5和R6都代表氢原子,或当R3、R4、R5和R6中的任何一个代表可被取代的甲基时,其他的代表氢原子。
4.根据权利要求3所述的二胺衍生物,其特征在于,R2和R7代表氢原子。
5.二胺衍生物,其由以下通式(9)表示:
其特征在于,R9代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的杂芳烷基、苯基、4位被取代的苯基或可被取代的杂芳基;
R10和R15独立地代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、具有3到6个碳原子的环烯基、具有2到6个碳原子的炔基、可被取代的芳烷基、可被取代的芳基或酰基;
R11和R12的中的一个代表甲基,另一个代表氢原子;
R13和R14分别代表氢原子;并且
R16代表苯基、4位被取代的苯基或可被取代的杂芳基。
6.根据权利要求5所述的二胺衍生物,其特征在于,
R9代表具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、具有2到6个碳原子的链烯基、可被取代的芳烷基、可被取代的杂芳烷基、苯基、4位被取代的苯基或可被取代的杂芳基;并且
R10和R15分别代表氢原子、具有1到6个碳原子的烷基、具有3到6个碳原子的环烷基、可被取代的芳烷基、可被取代的芳基或酰基。
7.根据权利要求6所述的二胺衍生物,其特征在于,R10和R15独立地代表氢原子、具有1到6个碳原子的烷基或酰基。
8.根据权利要求7所述的二胺衍生物,其特征在于,R10和R15分别代表氢原子。
9.杀菌剂,其特征在于,包括根据权利要求1到8中任一项所述的二胺衍生物作为其活性成分。
11.权利要求1的二胺衍生物的制备方法,其特征在于,具有通式(2)的化合物与具有以下通式(4)的化合物进行缩合,
其中,R8代表与权利要求1中的化合物的基团相同的基团。
14.权利要求5所述的二胺衍生物的制备方法,其特征在于,通式(10)的化合物与具有以下通式(12)的化合物进行缩合反应,
其中,R16代表与权利要求5中的化合物的基团相同的基团。
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WO2019001361A1 (zh) * | 2017-06-29 | 2019-01-03 | 沈阳中化农药化工研发有限公司 | 一种胡椒酸衍生物及其制备和应用 |
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CA2574217A1 (en) * | 2004-07-21 | 2006-01-26 | Mitsui Chemicals, Inc. | Diamine derivative, process of preparation thereof, and fungicide comprising diamine derivative as an active ingredient |
JP4520912B2 (ja) * | 2004-07-21 | 2010-08-11 | 三井化学アグロ株式会社 | ジアミン誘導体、その製造方法およびそれらを有効成分とする殺菌剤 |
JP2006219410A (ja) * | 2005-02-10 | 2006-08-24 | Mitsui Chemicals Inc | ジアミン誘導体、その製造方法およびそれらを有効成分とする殺菌剤 |
JP2006298785A (ja) * | 2005-04-18 | 2006-11-02 | Mitsui Chemicals Inc | ジアミン誘導体、その製造方法およびそれらを有効成分とする殺菌剤 |
JP4580836B2 (ja) * | 2005-07-25 | 2010-11-17 | 三井化学アグロ株式会社 | 殺虫殺菌組成物 |
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JP2010047478A (ja) * | 2006-12-19 | 2010-03-04 | Mitsui Chemicals Inc | 有害生物防除組成物 |
JP2010047479A (ja) * | 2006-12-19 | 2010-03-04 | Mitsui Chemicals Inc | 有害生物防除組成物 |
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CN105638697B (zh) * | 2014-12-02 | 2019-01-22 | 中化农化有限公司 | 含有甲氧基丙烯酸酯类杀菌剂的农药组合物及其应用 |
WO2019001361A1 (zh) * | 2017-06-29 | 2019-01-03 | 沈阳中化农药化工研发有限公司 | 一种胡椒酸衍生物及其制备和应用 |
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