一方面,本发明提供用于防治节肢动物、线虫、蠕虫和原虫害虫的化合物,所述的化合物具有下述通式:
其中
=X是=NR3、=O或电子对(在这种情况下,应理解为另一种代表式I的方式是删除=X);
R1是C1-C6烷基、C3-C6环烷基或C4-C8(环烷基)烷基,它们各任选由一或多个卤素取代;
R2和R3相互独立地选自:H;C1-C6烷基;C1-C6卤代烷基;COR4;S(O)pR4;CN;NO2;COOR4;CONR4R5;C(O)SR4;C(S)OR4;SO2NR4R5;P(O)q(R4)(R5);P(O)q(OR4)(R5);P(O)q(OR4)(OR5);C=(NR4)NR5R6;CH=NR4;C=(NR4)(OR5);C(S)N(R4)(R5);C(O)C(O)R4;C(O)C(O)OR4;C(O)C(O)NR4R5;和CONR4SO2R5;
m是1或2;
p是0、1或2;
q是0或1;R4、R5和R6相互独立地选自H;NO2;CN;CHO;R14;苯基,它任选由一或多个下列基团取代:R14、卤素、CN、NO2、OR14、SR14、COR14、COOR14或OR14;卤素;COR14;COOR14;CHO;和OH;
R7是CN、NO2、H、C1-C4烷基、C1-C4卤代烷基、卤素、CHO或COR20;
R8是H、卤素、CN、S(O)pR14、OR14、NR16R17、N(R16)CON(R17)(R18)、N3或由一或多个下列基团取代的NH(C1-C5烷基):OH、OR14、S(O)pR14、CN、NO2、COOR1或CON(R16)(R17);
R9和R11相互独立地选自:H、卤素、R14、OR14、SR14和R14;
R10是CN;
R
12是H、卤素、R
14、OR
14、S(O)
pR
14或
R13是H、卤素或R14;
Ar是苯基、任选带有一或多个选自卤素、R14、OR15、SF5和S(O)pR15的取代基;或Ar是2-吡啶基,任选带有一或多个选自卤素、R15、OR15、SF5和S(O)pR15的取代基;
R14和R19相互独立地选自:C1-C6烷基、C3-C6环烷基和C4-C8(环烷基)烷基,它们各任选由一或多个卤素取代;
R15是C1-C6烷基,任选由一或多个卤素取代;
R16、R17和R18相互独立地选自:H、NO2、CN、CHO、R19、COR19和COOR19;
R20选自C1-C6-烷基,任选由一或多个卤素取代;和
Z是阴离子抗衡离子,如Cl-、Br-、I-、F-、OSO2R4、ClO4-、OCOR-、BF4 -、SbF6 -、SO3 -或HSO4 -,磷酸根阴离子(phosphate anion)或磷酸氢根阴离子(hydrogenophosphate anion)或其它农业上可接受的阴离子。
式(I)或式(II)的立体异构体,例如非对映异构体或光学异构体也包括于本发明中。
本发明优选的化合物包括一或多个下列特点:
(1)R1是任选卤代的C1-C6烷基,优选是甲基或乙基;和/或
(2)R2是H、COOR4、S(O)pR4、CONR4R5、CN、COR4、P(O)q(OR4)(OR5)、P(O)q(R4)(R5);更优选的是,R2是H或CN或COOR4(其中R4是C1-C6烷基);或R2是S(O)pR4(其中p是2且R4是C1-C6烷基或任选取代的苯基);或R2是CONR4R5(其中R4是H或C1-C6烷基且是R5是C1-C6烷基,或其中R4是H且R5是COR14(其中R14是任选卤代的C1-C6烷基);或R2是COR4(其中R4是H或C1-C6-烷基);或R2是P(O)q(OR4)(OR5)或P(O)q(R4)(R5)(其中q是1且R4和R5各是C1-C6烷基);和/或
(3)Q是Q-1,优选其中R7是CN或H或C1-C4烷基和/或其中R8是N(R16)(R17),最优选其中R8是NH2;和/或
(4)Ar是苯基,该苯基在2位和6位由卤素取代和在4位上由卤代的C1-C6烷基或SF5或OR15取代,优选的是,Ar是2,6-二氯-4-三氟甲基苯基;或Ar是2-吡啶基,该吡啶基在3位上由卤素取代或在5位上由卤代C1-C6-烷基或SF5或OR15取代,优选的是Ar是3-氯-5-三氟甲基吡啶-2-基。
另一方面,本发明提供杀虫组合物(即,杀节肢动物、杀线虫、抗蠕虫或抗原虫组合物)包含杀虫有效量的(即,杀节肢动物有效量、杀线虫有效量、抗蠕虫有效量或抗原虫有效量)的式(I)或(II)化合物和其农业上可接受的盐。用于此及整个申请中的“式(I)或(II)化合物”的表述将式(I)或(II)及其盐的各种立体异构体形式包括在其范围内。
再一方面,本发明提供在一地点防治节肢动物、线虫、蠕虫或原虫的方法,所述的方法包含向所述的地点施用杀虫有效量(即,杀节肢动物有效量、杀线虫有效量、抗蠕虫有效量或抗原虫有效量)的式(I)或(II)化合物或上面定义的杀虫组合物。
式(I)(其中X是O且R2不是H)化合物由式(I)(其中X是电子对且R2不是H)化合物[所述的式(I)化合物也是本发明的一部分]通过本领域技术人员本身已知的方法,将硫原子氧化成亚砜亚胺基团而制备。这种转变可以用各种氧化剂,包括(但不限于)过锰酸钾、高碘酸钠和四氧化钌。可以在普通的溶剂如水、醚类例如二噁烷、腈类例如乙腈,或卤代烃如二氯甲烷、氯仿、四氯化碳等中,在约-100℃至约100℃间的温度下,优选在约0℃至约50℃下进行这种转变。这些化学方法可类似于见于(《四面体》[Tetrahedron],1975,31,305)的方法。
式(I)化合物(其中X是电子对且R2不是氢)可以由式(II)化合物,在碱存在下,通过与适宜的亲电试剂R2-L反应而制备。R2具有上面给出的含意,只是它不是H,且L是离去基团。离去基团L的实例是卤离子、乙酸根、苯基磺酸根、烷基磺酸根和苯氧基基团。可以用于反应的碱的实例是氢化钠、三乙胺和叔丁醇钾。
这些反应可以在各种普通的溶剂中进行,溶剂如(但不限于)醚类如四氢呋喃或二噁烷;水;卤代烃类如二氯甲烷或氯仿;腈类如乙腈等等。这些反应可以在约-100℃至100℃间的温度下进行,但优选在约0℃至溶剂的沸点温度下。
式(I)化合物(其中X是电子对且其中R2是H)可以通过常规的水解,由相应的式(I)化合物(其中R2是成酯基团COOR14)制备。
式(II)化合物可以根据本领域技术人员已知的方法,由式(III)化合物胺化而制备。
此化学法可以通过将式(III)的硫化物与胺化试剂混合来进行。所述的胺化试剂例如(但不限于)O-苯甲酰基羟胺,例如O-(2,4,6-三甲基苯甲酰基)羟胺或O-(3-氯苯甲酰基)羟胺;O-磺酰基羟胺如(但不限于)羟胺磺酸或O-(2,4,6-三异丙基苯磺酰基)羟胺;或O-氧膦基羟胺(O-phosphinic hydroxylamine)如O-(二苯基氧膦基)羟胺。此方法可以在各种溶剂中进行,溶剂包括(但不限于)水、卤代烃如二氯甲烷、氯仿、二氯乙烷等,和芳族溶剂如苯、甲苯、二甲苯类等,且可以在约-100℃至约100℃之间的温度下进行,优选在0℃至溶剂的沸点温度之间的温度下进行。此化学法类似于见于A/drichimicaActa,1980,13(1)3)中的方法。
式(I)(其中X是NH且R2是H)化合物可以可以通过式(III)化合物与氯胺反应而制备[《四面体》[Tetrahedron],1970,51,4449]。此反应可以在氨中,在约-100℃至-33℃之间的温度下进行。
式(I)[其中=X是=NR3(其中R3是如上所定义,只是它不是氢)且R2是H]化合物,可以通过在碱存在下,由式(I)(其中=X是NH且R2是H)化合物与适宜的亲电试剂R3-L反应而获得。R3如上所定义,只是它不是氢,且L是离去基团。离去基团L的实例是卤离子、乙酸根、苯基磺酸根、烷基磺酸根和苯氧基基团。可以用于反应的碱的实例是氢化钠、三乙胺和叔丁醇钾。
这些反应可以在各种普通溶剂中进行,溶剂例如(但不限于)醚类如四氢呋喃或二噁烷;水;卤代烃如二氯甲烷或氯仿;腈类如乙腈等。这些反应可以在约-100℃至约100℃之间的温度下进行,优选在0℃至溶剂的沸点温度之间的温度下进行。相似的反应可见于《比利时化学》((Chem.Ber),1984,117,2779)。
式(I)(其中(=X是=NR3其中R2和R3相同且均不是氢)化合物可以在碱存在下,由式(I)(其中R2是H且X是NH)化合物与至少二当量的适宜的亲电试剂R3-L反应而获得。R3具有上文中给定的含意,只是不是氢,且L是离去基团。离去基团L的实例是卤离子、乙酸根、苯基磺酸根、烷基磺酸根和苯氧基基团。可以用于反应的碱的实例是氢化钠、三乙胺和叔丁醇钾。
这些反应可以在各种普通溶剂中进行,溶剂例如(但不限于)醚类如四氢呋喃或二噁烷;水;卤代烃如二氯甲烷或氯仿;腈类如乙腈等。这些反应可以在约-100℃至约100℃之间的温度下进行,优选在0℃至溶剂之间的沸点温度下进行。相似的反应可见于(Lieb.Ann.Chem.,1972,759,107)。
式(III)化合物是本领域已知的。例如其中Q是Q-1的那些化合物描述于下列文献中:欧洲专利公开418016;欧洲专利公开403309;美国专利5,104,994;欧洲专利公开EP 352944;美国专利5,079,370;美国专利5,047,550;美国专利5,232,940;美国专利4,810,720;美国专利4,804,675;美国专利5,306,694;美国专利4,614,533;WPO公开WO93/06089;和WPO公开WO94/21606。其中Q是Q-2的式(III)化合物描述于美国专利5,187,185中。其中Q是Q-3的化合物描述于美国专利5,223,525中。
在上文中描述的许多转变中,选择的取代基或许会偶而干预所构思的反应,这点是显而易见的。这些负面作用可以通过使用适宜的保护基团,阻止不利的副反应来避免。也可以不影响除那些欲改变的官能团之外的官能团的反应剂。具体地选择适宜的保护基团和试剂是本领域技术人员易于理解的。《美国化学文摘》[Chemical Abstracts]被认为且建议作为本领域技术人员的知识构成。
为进一步说明本发明及其优点,给出下列具体实施例,这些实施例应理解为只用作说明的目的,而非以任何方式限制本发明的范围。
实施例1
2,4,6-三甲基苯磺酸,与S-4-[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基]吡唑基-S-乙基硫亚胺的化合物:
O-亚基磺酰基乙酰氧肟酸乙酯(10克,0.035摩尔)溶解于二噁烷(10毫升)中,并冷却至0℃。加入70%的高氯酸(3.3毫升,0.038摩尔),并将混合物搅拌10分钟。加入水(200毫升),滤出余下的固体,用水洗涤,之后溶解于二氯甲烷(50毫升)中,并与水相分离。
将5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基-4-乙硫基吡唑(10.7克,0.028摩尔)溶解于二氯甲烷(50毫升)中,将所得的溶液冷却至0℃。加入上段中的溶液。在0℃且之后在室温下搅拌1小时后,去除二氯甲烷,加入乙醚(200毫升)。滤出所得的固体,给出标题化合物,为白色固体(12.45克,75%),熔点约193℃。
以相似的方式,制备下列化合物:2,4,6-三甲基苯磺酸,与S-4-[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基]吡唑基-S-甲基硫亚胺的化合物,熔点约180℃,下文称作实施例1a;2,4,6-三甲基苯磺酸,与S-4-[5-氨基-1-(2,6-二氯-4-三氟甲基)苯基]吡唑基-S-甲基硫亚胺的化合物,熔点约187℃,下文称作实施例1b。
下面的二个化合物也由上面的方法(但不分离)制备,用作实施例2:2,4,6-三甲基苯磺酸,与S-4-[5-氨基-1-(2,6-二氯-4-三氟甲基)苯基-3-甲基]吡唑基-S-乙基硫亚胺的化合物和2,4,6-三甲基苯磺酸,与S-4-[5-氨基-1-(2,6-二氯-4-三氟甲基)苯基-3-乙基]吡唑基-S-乙基硫亚胺的化合物。
实施例2
S-{[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基]-4-(1H-吡唑基)}-S-乙基-N-(叔丁氧基羰基)硫亚胺:
将实施例1的产物(1.0克,1.7毫摩尔)于二氯甲烷(10毫升)中搅拌,冷却至0℃,并加入三乙胺(1.2毫升,8.5毫摩尔)。加入二叔丁基二碳酸酯(0.6毫升,2.6毫摩尔),并将反应搅拌50分钟。混合物用乙醚稀释,用水(3×50毫升)和饱和氯化钠水溶液(75毫升)洗涤。将有机层干燥,过滤并浓缩。所得的油状物与冷戊烷混合,并滤出沉淀。将固体物与滤液合并,去除溶剂,使的油状物与冷戊烷混合,并滤出沉淀。将固体物与滤液合并,去除溶剂,使用2∶3的乙酸乙酯∶己烷作洗脱液,将油状物经硅胶过滤。去除溶剂后,由乙醚/戊烷沉淀,给出标题化合物,为白色固体(0.36克,43%),熔点约191℃。
用相似的方式,制备下列的化合物(表1)。
表1
实施例 #R
1 R
2 R
7 熔点3 Et COMe CN 约163℃4 Et COOMe CN 约200℃5 Et SO
2Me CN 约191℃6 Et CONHMe CN 约187℃7 Et CN CN 约175℃8 Et CHO CN 约181℃9 Me COMe CN 约159℃10 Et PO(OEt)
2 CN 胶11 Et CON(Me)
2 CN 约173℃12 Et PO(Me)
2 CN 约150℃13 Et CONHCOCCl
3 CN 约116℃14 Et CONHCOCH
2Cl CN 约159℃15 Et C(S)NHMe CN 约90℃
表1(续)实施例 #R1 R2 R7 熔点16 Et CONHCH2COOEt CN 约91℃17 Me C(S)NHMe CN 约95℃18 Et CONHCOOEt CN 约167℃19 Me CHO CN 约160℃20 Me CN CN 约181℃21 Me C(O)C(O)Me CN 约204℃22 Me COOtBu CN 约196℃23 Me CHO H 约199℃24 Me COMe H 约181℃25 Me CN H 约182℃26 Et CHO Me 约159℃27 Et CN Me 约67℃28 Et CHO Et 胶29 Et CN Et 约64℃
实施例30
N-(叔丁氧基羰基)-S-4-[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基吡唑基]-S-乙基亚砜亚胺:
将实施例2的产物(1.55克,31毫摩尔)溶解于1∶1的乙腈∶四氯化碳的混合物(19毫升)。加入偏高碘酸钠(2.7克,12.4毫摩尔)的水(19毫升)溶液。加入氯化钌(III)水合物(20毫克,用于原位产生四氧化物)和乙腈(25毫升)。2小时后,加入另一份高碘酸钠(1.8克,8.2毫摩尔)和氯化钌(III)水合物(15毫克,用于原位产生氧化物),并将反应搅拌30分钟。之后依次加入水(100毫升)和乙醚(100毫升)和异丙醇(2毫升),并混合。分离有机相,接着用水(100毫升)和饱和氯化钠水溶液(100毫升)洗涤。在经硫酸镁干燥后,将混合物过滤,去除溶剂,提供油状残留物,将之用冷乙醚和二氯甲烷研磨,给出标题化合物,为棕色胶状固体(0.94克,60%)。于CDCl3中的质子核磁共振谱具有下列化学位移:7.81(m,2H);5.57(brs,2H);3.7-3.5(m,2H);1.44(s,9H);1.39(t,3H)。
用相似的方式,制备出N-乙酰基-S-4-[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基吡唑基]-S-乙基亚砜亚胺(熔点约217℃),下文称作实施例30a。
实施例31
S-4-[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基吡唑基]-S-乙基亚砜亚胺:
将实施例30的产物(0.1克,0.2毫摩尔)溶解于2毫升乙腈中。将粉末状分子筛(0.1克)、碘化钠(0.07克,0.46毫摩尔)和氯三甲基硅烷(0.06毫升,0.46毫摩尔)合并于2毫升乙腈中,并将之加入至上述溶液中。25分钟后,将混合物用乙醚(7毫升)稀释,接着用水、10%盐酸水溶液和饱和氯化钠水溶液洗涤。有机相经硫酸钠干燥,过滤并减压浓缩。残留的油状物用冷戊烷和二氯甲烷研磨,留下所需的产物,为黄色固体(46毫克),熔点约86℃。
实施例32
S-[5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基)苯基-4-(1H-吡唑基)]-S-甲基-N-[(4-甲基苯基)磺酰基]硫亚胺:
向搅拌着的5-氨基-1-(2,6-二氯-4-三氟甲基)苯基-4-甲硫基-1H-吡唑-3-腈(0.99克,2.7毫摩尔)的乙腈(25毫升)溶液,经2分钟,加入N-氯-对甲苯磺酰胺钠盐水合物(Chloramine-T水合物)(0.61克,2.7毫摩尔)于水(5毫升)中的水溶液。搅拌于室温下继续大约2小时,之后将混合物用蒸汽浴加热至沸腾1小时。在减压下去除挥发物,并将残留物于硅胶上层析,洗脱用3∶1的乙酸乙酯/己烷,给出0.81克标题化合物,为固体,熔点约197℃。
实施例33
S-4-[5-氨基-3-氰基-1-(2-(3-氯5-三氟甲基)吡啶基)吡唑基]-S-乙基亚砜
将O-亚基磺酰基乙酰氧肟酸乙酯(0.47克,1.64毫摩尔)溶解于二噁烷(1毫升)中,并冷却至0℃。加入70%的高氯酸(0.5毫升),并将混合物搅拌10分钟。加入水中,滤出余下固体,用水洗涤,之后溶解于二氯甲烷中,并与水相分离。
将5-氨基-3-氰基-1-(2-(3-氯-5-三氟甲基)吡啶基)-4-乙基亚磺酰基吡唑(0.5克,1.37毫摩尔)溶解于二氯甲烷(25毫升),并将所得的溶液冷却至0℃。加入上段中的溶液。一月后,将混合物浓缩至固体,且反复洗涤,直到无原料吡唑留下。由此给出标题化合物,为白色固体,熔点约193℃。
进一步的说明性本发明具体化合物给出下列表格2-5中。在整个表中,标志“¨”用于表示单独电子对。
表2R1 R7 R8 NR2 XMe CN NH2 NCOEtMe CN NH2 NCOPrMe CN NH2 NCOiPrMe CN NH2 NCOtBuMe CN NH2 NCOPhMe CN NH2 NSO2EtMe CN NH2 NSO2PhMe CN NH2 NSO2PrMe CN NH2 NSO2iPrMe CN NH2 NNO2Me CN NH2 NCOOEtMe CN NH2 NCOOPh
表2(续)R1 R7 R8 NR2 XMe CN NH2 NCOOPrMe CN NH2 NCOOiPrMe CN NH2 NCONHEtMe CN NH2 NCONHPrMe CN NH2 NCONHiPr ¨Me CN NH2 NCOSMeMe CN NH2 NCOSEtMe CN NH2 NCSOMeMe CN NH2 NCSOEtMe CN NH2 NCSOPrMe CN NH2 NSO2NH2Me CN NH2 NSO2NHMeMe CN NH2 NSO2NMe2Me CN NH2 NP(O)(OMe)2Me CN NH2 NP(O)(OMe)(OMe)Me CN NH2 NP(O)(OPr)2Me CN NH2 NP(O)(Et)2Me CN NH2 NC(O)C(O)HMe CN NH2 NC(O)C(O)MeMe CN NH2 NC(O)C(O)OMeMe CN NH2 NC(O)C(O)OEtMe CN NH2 NC(O)C(O)NH2Me CN NH2 NC(O)C(O)OHMe CN NH2 NC(NH)NH2Me CN NH2 NC(NOH)NH2Me CN NH2 NC(NH)NHMeMe CN NH2 NC(NH)NMe2Me CN NH2 NC(NH)OMe ¨Me CN NH2 NC(NH)OEtEt CN NH2 NCOEtEt CN NH2 NCOPr ¨Et CN NH2 NCOiPr ¨Et CN NH2 NCOtBu ¨Et CN NH2 NCOPhEt CN NH2 NSO2EtEt CN NH2 NSO2PhEt CN NH2 NSO2PrEt CN NH2 NSO2iPrEt CN NH2 NNO2Et CN NH2 NCOOEtEt CN NH2 NCOOPhEt CN NH2 NCOOPrEt CN NH2 NCOOiPrEt CN NH2 NCONHEtEt CN NH2 NCONHPrEt CN NH2 NCONHiPrEt CN NH2 NCOSMeEt CN NH2 NCOSEtEt CN NH2 NCSOMeEt CN NH2 NCSOEtEt CN NH2 NCSOPrEt CN NH2 NSO2NH2Et CN NH2 NSO2NHMeEt CN NH2 NSO2NMe2Et CN NH2 NP(O)(OMe)2Et CN NH2 NP(O)(OMe)(OMe)Et CN NH2 NP(O)(OPr)2Et CN NH2 NP(O)(Et)2 ¨Et CN NH2 NC(O)C(O)H ¨Et CN NH2 NC(O)C(O)Me ¨Et CN NH2 NC(O)C(O)OMe ¨Et CN NH2 NC(O)C(O)OEtEt CN NH2 NC(O)C(O)NH2Et CN NH2 NC(O)C(O)OHEt CN NH2 NC(NH)NH2Et CN NH2 NC(NOH)NH2Et CN NH2 NC(NH)NHMeEt CN NH2 NC(NH)NMe2Et CN NH2 NC(NH)OMeEt CN NH2 NC(NH)OEtMe CN NHMe NCOMeMe CN NHMe NCOEtMe CN NHMe NCOPrMe CN NHMe NCHOMe CN NHMe NCOiPrMe CN NHMe NCOtBuMe CN NHMe NCOPhMe CN NHMe NSO2MeMe CN NHMe NSO2EtMe CN NHMe NSO2PrMe CN NHMe NSO2PhMe CN NHMe NSO2iPrMe CN NHMe NNO2Me CN NHMe NCOOMeMe CN NHMe NCOOEt ¨Me CN NHMe NCOOPr ¨Me CN NHMe NCOOiPr ¨Me CN NHMe NCONHEt ¨Me CN NHMe NCONHPr ¨Me CN NHMe NCONH2 ¨Me CN NHMe NCONHMeMe CN NHMe NCNMe CN NHMe NCOSMeMe CN NHMe NCOSEtMe CN NHMe NCSOMeMe CN NHMe NCSOEtMe CN NHMe NCSOPrMe CN NHMe NSO2NH2Me CN NHMe NSO2NHMeMe CN NHMe NSO2NMe2Me CN NHMe NP(O)(OMe)2Me CN NHMe NP(O)(OEt)2Me CN NHMe NP(O)Me2Me CN NHMe NP(O)Et2Me CN NHMe NP(O)Me(OMe)Me CN NHMe NP(O)(OPr)2Me CN NHMe NC(O)C(O)HMe CN NHMe NC(O)C(O)MeMe CN NHMe NC(O)C(O)OMeMe CN NHMe NC(O)C(O)OEtMe CN NHMe NC(O)C(O)NH2Me CN NHMe NC(O)C(O)OHMe CN NHMe NC(NH)NH2Me CN NHMe NC(NOH)NH2Me CN NHMe NC(NH)NHMe ¨Me CN NHMe NC(NH)NMe2 ¨Me CN NHMe NC(NH)OMe ¨Me CN NHMe NC(NH)OEtMe CN NHEt NCOMeMe CN NHEt NCOEtMe CN NHEt NCOPrMe CN NHEt NCHOMe CN NHEt NCOiPrMe CN NHEt NCOtBuMe CN NHEt NCOPhMe CN NHEt NSO2MeMe CN NHEt NSO2EtMe CN NHEt NSO2PrMe CN NHEt NSO2PhMe CN NHEt NSO2iPrMe CN NHEt NNO2Me CN NHEt NCOOMeMe CN NHEt NCOOEtMe CN NHEt NCOOPrMe CN NHEt NCOOiPrMe CN NHEt NCONHEtMe CN NHEt NCONHPrMe CN NHEt NCONH2Me CN NHEt NCONHMeMe CN NHEt NCNMe CN NHEt NCOSMe ¨Me CN NHEt NCOSEt ¨Me CN NHEt NCSOMeMe CN NHEt NCSOEt ¨Me CN NHEt NCSOPr ¨Me CN NHEt NSO2NH2Me CN NHEt NSO2NHMeMe CN NHEt NSO2NMe2Me CN NHEt NP(O)(OMe)2Me CN NHEt NP(O)(OEt)2Me CN NHEt NP(O)Me2Me CN NHEt NP(O)Et2Me CN NHEt NP(O)Me(OMe)Me CN NHEt NP(O)(OPr)2Me CN NHEt NC(O)C(O)HMe CN NHEt NC(O)C(O)MeMe CN NHEt NC(O)C(O)OMeMe CN NHEt NC(O)C(O)OEtMe CN NHEt NC(O)C(O)NH2Me CN NHEt NC(O)C(O)OHMe CN NHEt NC(NH)NH2Me CN NHEt NC(NOH)NH2Me CN NHEt NC(NH)NHMeMe CN NHEt NC(NH)NMe2Me CN NHEt NC(NH)OMeMe CN NHEt NC(NH)OEtMe CN NHPr NCOMeMe CN NHPr NCOEtMe CN NHPr NCOPrMe CN NHPr NCHOMe CN NHPr NCOiPrMe CN NHPr NCOtBuMe CN NHPr NCOPhMe CN NHPr NSO2MeMe CN NHPr NSO2EtMe CN NHPr NSO2PrMe CN NHPr NSO2PhMe CN NHPr NSO2iPrMe CN NHPr NNO2Me CN NHPr NCOOMeMe CN NHPr NCOOEtMe CN NHPr NCOOPrMe CN NHPr NCOOiPrMe CN NHPr NCONHEtMe CN NHPr NCONHPrMe CN NHPr NCONH2Me CN NHPr NCONHMeMe CN NHPr NCNMe CN NHPr NCOSMeMe CN NHPr NCOSEtMe CN NHPr NCSOMeMe CN NHPr NCSOEtMe CN NHPr NCSOPrMe CN NHPr NSO2NH2Me CN NHPr NSO2NHMeMe CN NHPr NSO2NMe2Me CN NHPr NP(O)(OMe)2Me CN NHPr NP(O)(OEt)2Me CN NHPr NP(O)Me2Me CN NHPr NP(O)Et2Me CN NHPr NP(O)Me(OMe)Me CN NHPr NP(O)(OPr)2Me CN NHPr NC(O)C(O)HMe CN NHPr NC(O)C(O)MeMe CN NHPr NC(O)C(O)OMeMe CN NHPr NC(O)C(O)OEtMe CN NHPr NC(O)C(O)NH2Me CN NHPr NC(O)C(O)OHMe CN NHPr NC(NH)NH2Me CN NHPr NC(NOH)NH2Me CN NHPr NC(NH)NHMeMe CN NHPr NC(NH)NMe2Me CN NHPr NC(NH)OMeMe CN NHPr NC(NH)OEtEt CN NHMe NCOMeEt CN NHMe NCOEtEt CN NHMe NCOPrEt CN NHMe NCHOEt CN NHMe NCOiPrEt CN NHMe NCOtBuEt CN NHMe NCOPhEt CN NHMe NSO2MeEt CN NHMe NSO2EtEt CN NHMe NSO2PrEt CN NHMe NSO2PhEt CN NHMe NSO2iPrEt CN NHMe NNO2 ¨Et CN NHMe NCOOMeEt CN NHMe NCOOEtEt CN NHMe NCOOPrEt CN NHMe NCOOiPrEt CN NHMe NCONHEtEt CN NHMe NCONHPrEt CN NHMe NCONH2Et CN NHMe NCONHMeEt CN NHMe NCNEt CN NHMe NCOSMeEt CN NHMe NCOSEtEt CN NHMe NCSOMeEt CN NHMe NCSOEtEt CN NHMe NCSOPrEt CN NHMe NSO2NH2Et CN NHMe NSO2NHMeEt CN NHMe NSO2NMe2Et CN NHMe NP(O)(OMe)2Et CN NHMe NP(O)(OEt)2Et CN NHMe NP(O)Me2Et CN NHMe NP(O)Et2Et CN NHMe NP(O)Me(OMe)Et CN NHMe NP(O)(OPr)2Et CN NHMe NC(O)C(O)H ¨Et CN NHMe NC(O)C(O)Me ¨Et CN NHMe NC(O)C(O)OMe ¨Et CN NHMe NC(O)C(O)OEtEt CN NHMe NC(O)C(O)NH2Et CN NHMe NC(O)C(O)OH ¨Et CN NHMe NC(NH)NH2 ¨Et CN NHMe NC(NOH)NH2Et CN NHMe NC(NH)NHMeEt CN NHMe NC(NH)NMe2Et CN NHMe NC(NH)OMeEt CN NHMe NC(NH)OEtEt CN NHEt NCOMeEt CN NHEt NCOEtEt CN NHEt NCOPrEt CN NHEt NCHOEt CN NHEt NCOiPrEt CN NHEt NCOtBuEt CN NHEt NCOPhEt CN NHEt NSO2MeEt CN NHEt NSO2EtEt CN NHEt NSO2PrEt CN NHEt NSO2PhEt CN NHEt NSO2iPrEt CN NHEt NNO2Et CN NHEt NCOOMeEt CN NHEt NCOOEtEt CN NHEt NCOOPrEt CN NHEt NCOOiPrEt CN NHEt NCONHEtEt CN NHEt NCONHPr ¨Et CN NHEt NCONH2Et CN NHEt NCONHMe ¨Et CN NHEt NCN ¨Et CN NHEt NCOSMe ¨Et CN NHEt NCOSEtEt CN NHEt NCSOMeEt CN NHEt NCSOEtEt CN NHEt NCSOPrEt CN NHEt NSO2NH2Et CN NHEt NSO2NHMeEt CN NHEt NSO2NMe2Et CN NHEt NP(O)(OMe)2Et CN NHEt NP(O)(OEt)2Et CN NHEt NP(O)Me2Et CN NHEt NP(O)Et2Et CN NHEt NP(O)Me(OMe)Et CN NHEt NP(O)(OPr)2Et CN NHEt NC(O)C(O)HEt CN NHEt NC(O)C(O)MeEt CN NHEt NC(O)C(O)OMeEt CN NHEt NC(O)C(O)OEtEt CN NHEt NC(O)C(O)NH2Et CN NHEt NC(O)C(O)OHEt CN NHEt NC(NH)NH2Et CN NHEt NC(NOH)NH2Et CN NHEt NC(NH)NHMeEt CN NHEt NC(NH)NMe2Et CN NHEt NC(NH)OMeEt CN NHEt NC(NH)OEtEt CN NHPr NCOMeEt CN NHPr NCOEtEt CN NHPr NCOPrEt CN NHPr NCHOEt CN NHPr NCOiPrEt CN NHPr NCOtBuEt CN NHPr NCOPhEt CN NHPr NSO2MeEt CN NHPr NSO2EtEt CN NHPr NSO2PrEt CN NHPr NSO2PhEt CN NHPr NSO2iPrEt CN NHPr NNO2Et CN NHPr NCOOMeEt CN NHPr NCOOEtEt CN NHPr NCOOPrEt CN NHPr NCOOiPrEt CN NHPr NCONHEtEt CN NHPr NCONHPrEt CN NHPr NCONH2Et CN NHPr NCONHMeEt CN NHPr NCNEt CN NHPr NCOSMeEt CN NHPr NCOSEtEt CN NHPr NCSOMeEt CN NHPr NCSOEtEt CN NHPr NCSOPr ¨Et CN NHPr NSO2NH2 ¨Et CN NHPr NSO2NHMe ¨Et CN NHPr NSO2NMe2 ¨Et CN NHPr NP(O)(OMe)2 ¨Et CN NHPr NP(O)(OEt)2Et CN NHPr NP(O)Me2Et CN NHPr NP(O)Et2Et CN NHPr NP(O)Me(OMe)Et CN NHPr NP(O)(OPr)2Et CN NHPr NC(O)C(O)HEt CN NHPr NC(O)C(O)MeEt CN NHPr NC(O)C(O)OMeEt CN NHPr NC(O)C(O)OEtEt CN NHPr NC(O)C(O)NH2Et CN NHPr NC(O)C(O)OHEt CN NHPr NC(NH)NH2Et CN NHPr NC(NOH)NH2Et CN NHPr NC(NH)NHMeEt CN NHPr NC(NH)NMe2Et CN NHPr NC(NH)OMeEt CN NHPr NC(NH)OEtMe CN NH2 NCOMe OMe CN NH2 NCOEt OMe CN NH2 NCOPr OMe CN NH2 NCHO OMe CN NH2 NCOiPr OMe CN NH2 NCOtBu OMe CN NH2 NCOPh OMe CN NH2 NSO2Me OMe CN NH2 NSO2Et OMe CN NH2 NSO2Pr OMe CN NH2 NSO2Ph OMe CN NH2 NSO2iPr OMe CN NH2 NNO2 OMe CN NH2 NCOOMe OMe CN NH2 NCOOEt OMe CN NH2 NCOOPr OMe CN NH2 NCOOiPr OMe CN NH2 NCONHEt OMe CN NH2 NCONHPr OMe CN NH2 NCONH2 OMe CN NH2 NCONHMe OMe CN NH2 NCN OMe CN NH2 NCOSMe OMe CN NH2 NCOSEt OMe CN NH2 NCSOMe OMe CN NH2 NCSOEt OMe CN NH2 NCSOPr OMe CN NH2 NSO2NH2 OMe CN NH2 NSO2NHMe OMe CN NH2 NSO2NMe2 OMe CN NH2 NP(O)(OMe)2 OMe CN NH2 NP(O)(OEt)2 OMe CN NH2 NP(O)Me2 OMe CN NH2 NP(O)Et2 OMe CN NH2 NP(O)Me(OMe) OMe CN NH2 NP(O)(OPr)2 OMe CN NH2 NC(O)C(O)H OMe CN NH2 NC(O)C(O)Me OMe CN NH2 NC(O)C(O)OMe OMe CN NH2 NC(O)C(O)OEt OMe CN NH2 NC(O)C(O)NH2 OMe CN NH2 NC(O)C(O)OH OMe CN NH2 NC(NH)NH2 OMe CN NH2 NC(NOH)NH2 OMe CN NH2 NC(NH)NHMe OMe CN NH2 NC(NH)NMe2 OMe CN NH2 NC(NH)OMe OMe CN NH2 NC(NH)OEt OMe CN NH2 NH OMe CN NHMe NCOMe OMe CN NHMe NCOEt OMe CN NHMe NCOPr OMe CN NHMe NCHO OMe CN NHMe NCOiPr OMe CN NHMe NCOtBu OMe CN NHMe NCOPh OMe CN NHMe NSO2Me OMe CN NHMe NSO2Et OMe CN NHMe NSO2Pr OMe CN NHMe NSO2Ph OMe CN NHMe NSO2iPr OMe CN NHMe NNO2 OMe CN NHMe NCOOMe OMe CN NHMe NCOOEt OMe CN NHMe NCOOPr OMe CN NHMe NCOOiPr OMe CN NHMe NCONHEt OMe CN NHMe NCONHPr OMe CN NHMe NCONH2 OMe CN NHMe NCONHMe OMe CN NHMe NCN OMe CN NHMe NCOSMe OMe CN NHMe NCOSEt OMe CN NHMe NCSOMe OMe CN NHMe NCSOEt OMe CN NHMe NCSOPr OMe CN NHMe NSO2NH2 OMe CN NHMe NSO2NHMe OMe CN NHMe NSO2NMe2 OMe CN NHMe NP(O)(OMe)2 OMe CN NHMe NP(O)(OEt)2 OMe CN NHMe NP(O)Me2 OMe CN NHMe NP(O)Et2 OMe CN NHMe NP(O)Me(OMe) OMe CN NHMe NP(O)(OPr)2 OMe CN NHMe NC(O)C(O)H OMe CN NHMe NC(O)C(O)Me OMe CN NHMe NC(O)C(O)OMe OMe CN NHMe NC(O)C(O)OEt OMe CN NHMe NC(O)C(O)NH2 OMe CN NHMe NC(O)C(O)OH OMe CN NHMe NC(NH)NH2 OMe CN NHMe NC(NOH)NH2 OMe CN NHMe NC(NH)NHMe OMe CN NHMe NC(NH)NMe2 OMe CN NHMe NC(NH)OMe OMe CN NHMe NC(NH)OEt OMe CN NHEt NCOMe OMe CN NHEt NCOEt OMe CN NHEt NCOPr OMe CN NHEt NCHO OMe CN NHEt NCOiPr OMe CN NHEt NCOtBu OMe CN NHEt NCOPh OMe CN NHEt NSO2Me OMe CN NHEt NSO2Et OMe CN NHEt NSO2Pr OMe CN NHEt NSO2Ph OMe CN NHEt NSO2iPr OMe CN NHEt NNO2 OMe CN NHEt NCOOMe OMe CN NHEt NCOOEt OMe CN NHEt NCOOPr OMe CN NHEt NCOOiPr OMe CN NHEt NCONHEt OMe CN NHEt NCONHPr OMe CN NHEt NCONH2 OMe CN NHEt NCONHMe OMe CN NHEt NCN OMe CN NHEt NCOSMe OMe CN NHEt NCOSEt OMe CN NHEt NCSOMe OMe CN NHEt NCSOEt OMe CN NHEt NCSOPr OMe CN NHEt NSO2NH2 OMe CN NHEt NSO2NHMe OMe CN NHEt NSO2NMe2 OMe CN NHEt NP(O)(OMe)2 OMe CN NHEt NP(O)(OEt)2 OMe CN NHEt NP(O)Me2 OMe CN NHEt NP(O)Et2 OMe CN NHEt NP(O)Me(OMe) OMe CN NHEt NP(O)(OPr)2 OMe CN NHEt NC(O)C(O)H OMe CN NHEt NC(O)C(O)Me OMe CN NHEt NC(O)C(O)OMe OMe CN NHEt NC(O)C(O)OEt OMe CN NHEt NC(O)C(O)NH2 OMe CN NHEt NC(O)C(O)OH OMe CN NHEt NC(NH)NH2 OMe CN NHEt NC(NOH)NH2 OMe CN NHEt NC(NH)NHMe OMe CN NHEt NC(NH)NMe2 OMe CN NHEt NC(NH)OMe OMe CN NHEt NC(NH)OEt OEt CN NH2 NCOEt OEt CN NH2 NCOPr OEt CN NH2 NCHO OEt CN NH2 NCOiPr OEt CN NH2 NCOtBu OEt CN NH2 NCOPh OEt CN NH2 NSO2Me OEt CN NH2 NSO2Et OEt CN NH2 NSO2Pr OEt CN NH2 NSO2Ph OEt CN NH2 NSO2iPr OEt CN NH2 NNO2 OEt CN NH2 NCOOMe OEt CN NH2 NCOOEt OEt CN NH2 NCOOPr OEt CN NH2 NCOOiPr OEt CN NH2 NCONHEt OEt CN NH2 NCONHPr OEt CN NH2 NCONH2 OEt CN NH2 NCONHMe OEt CN NH2 NCN OEt CN NH2 NCOSMe OEt CN NH2 NCOSEt OEt CN NH2 NCSOMe OEt CN NH2 NCSOEt OEt CN NH2 NCSOPr OEt CN NH2 NSO2NH2 OEt CN NH2 NSO2NHMe OEt CN NH2 NSO2NMe2 OEt CN NH2 NP(O)(OMe)2 OEt CN NH2 NP(O)(OEt)2 OEt CN NH2 NP(O)Me2 OEt CN NH2 NP(O)Et2 OEt CN NH2 NP(O)Me(OMe) OEt CN NH2 NP(O)(OPr)2 OEt CN NH2 NC(O)C(O)H OEt CN NH2 NC(O)C(O)Me OEt CN NH2 NC(O)C(O)OMe OEt CN NH2 NC(O)C(O)OEt OEt CN NH2 NC(O)C(O)NH2 OEt CN NH2 NC(O)C(O)OH OEt CN NH2 NC(NH)NH2 OEt CN NH2 NC(NOH)NH2 OEt CN NH2 NC(NH)NHMe OEt CN NH2 NC(NH)NMe2 OEt CN NH2 NC(NH)OMe OEt CN NH2 NC(NH)OEt OEt CN NHMe NH OEt CN NHMe NCOMe OEt CN NHMe NCOEt OEt CN NHMe NCOPr OEt CN NHMe NCHO OEt CN NHMe NCOiPr OEt CN NHMe NCOtBu OEt CN NHMe NCOPh OEt CN NHMe NSO2Me OEt CN NHMe NSO2Et OEt CN NHMe NSO2Pr OEt CN NHMe NSO2Ph OEt CN NHMe NSO2iPr OEt CN NHMe NNO2 OEt CN NHMe NCOOMe OEt CN NHMe NCOOEt OEt CN NHMe NCOOPr OEt CN NHMe NCOOiPr OEt CN NHMe NCONHEt OEt CN NHMe NCONHPr OEt CN NHMe NCONH2 OEt CN NHMe NCONHMe OEt CN NHMe NCN OEt CN NHMe NCOSMe OEt CN NHMe NCOSEt OEt CN NHMe NCSOMe OEt CN NHMe NCSOEt OEt CN NHMe NCSOPr OEt CN NHMe NSO2NH2 OEt CN NHMe NSO2NHMe OEt CN NHMe NSO2NMe2 OEt CN NHMe NP(O)(OMe)2 OEt CN NHMe NP(O)(OEt)2 OEt CN NHMe NP(O)Me2 OEt CN NHMe NP(O)Et2 OEt CN NHMe NP(O)Me(OMe) OEt CN NHMe NP(O)(OPr)2 OEt CN NHMe NC(O)C(O)H OEt CN NHMe NC(O)C(O)Me OEt CN NHMe NC(O)C(O)OMe OEt CN NHMe NC(O)C(O)OEt OEt CN NHMe NC(O)C(O)NH2 OEt CN NHMe NC(O)C(O)OH OEt CN NHMe NC(NH)NH2 OEt CN NHMe NC(NOH)NH2 OEt CN NHMe NC(NH)NHMe OEt CN NHMe NC(NH)NMe2 OEt CN NHMe NC(NH)OMe OEt CN NHMe NC(NH)OEt OEt CN NHEt NCOMe OEt CN NHEt NCOEt OEt CN NHEt NCOPr OEt CN NHEt NCHO OEt CN NHEt NCOiPr OEt CN NHEt NCOtBu OEt CN NHEt NCOPh OEt CN NHEt NSO2Me OEt CN NHEt NSO2Et OEt CN NHEt NSO2Pr OEt CN NHEt NSO2Ph OEt CN NHEt NSO2iPr OEt CN NHEt NNO2 OEt CN NHEt NCOOMe OEt CN NHEt NCOOEt OEt CN NHEt NCOOPr OEt CN NHEt NCOOiPr OEt CN NHEt NCONHEt OEt CN NHEt NCONHPr OEt CN NHEt NCONH2 OEt CN NHEt NCONHMe OEt CN NHEt NCN OEt CN NHEt NCOSMe OEt CN NHEt NCOSEt OEt CN NHEt NCSOMe OEt CN NHEt NCSOEt OEt CN NHEt NCSOPr OEt CN NHEt NSO2NH2 OEt CN NHEt NSO2NHMe OEt CN NHEt NSO2NMe2 OEt CN NHEt NP(O)(OMe)2 OEt CN NHEt NP(O)(OEt)2 OEt CN NHEt NP(O)Me2 OEt CN NHEt NP(O)Et2 OEt CN NHEt NP(O)Me(OMe) OEt CN NHEt NP(O)(OPr)2 OEt CN NHEt NC(O)C(O)H OEt CN NHEt NC(O)C(O)Me OEt CN NHEt NC(O)C(O)OMe OEt CN NHEt NC(O)C(O)OEt OEt CN NHEt NC(O)C(O)NH2 OEt CN NHEt NC(O)C(O)OH OEt CN NHEt NC(NH)NH2 OEt CN NHEt NC(NOH)NH2 OEt CN NHEt NC(NH)NHMe OEt CN NHEt NC(NH)NMe2 OEt CN NHEt NC(NH)OMe OEt CN NHEt NC(NH)OEt OMe CN NHCOMe NCOMeMe CN NHCOMe NCOEtMe CN NHCOMe NCOPrMe CN NHCOMe NCHOMe CN NHCOMe NCOiPrMe CN NHCOMe NCOtBuMe CN NHCOMe NCOPhMe CN NHCOMe NSO2MeMe CN NHCOMe NSO2EtMe CN NHCOMe NSO2PrMe CN NHCOMe NSO2PhMe CN NHCOMe NSO2iPrMe CN NHCOMe NNO2Me CN NHCOMe NCOOMeMe CN NHCOMe NCOOEtMe CN NHCOMe NCOOPrMe CN NHCOMe NCOOiPrMe CN NHCOMe NCONHFMe CN NHCOMe NCONHPrMe CN NHCOMe NCONH2Me CN NHCOMe NCONHMeMe CN NHCOMe NCNMe CN NHCOMe NCOSMeMe CN NHCOMe NCOSEtMe CN NHCOMe NCSOMe ¨Me CN NHCOMe NCSOEtMe CN NHCOMe NCSOPr ¨Me CN NHCOMe NSO2NH2 ¨Me CN NHCOMe NSO2NHMe ¨Me CN NHCOMe NSO2NMe2 ¨Me CN NHCOMe NP(O)(OMe)2 ¨Me CN NHCOMe NP(O)(OEt)2 ¨Me CN NHCOMe NP(O)Me2Me CN NHCOMe NP(O)Et2Me CN NHCOMe NP(O)Me(OMe) ¨Me CN NHCOMe NP(O)(OPr)2Me CN NHCOMe NC(O)C(O)H ¨Me CN NHCOMe NC(O)C(O)MeMe CN NHCOMe NC(O)C(O)OMeMe CN NHCOMe NC(O)C(O)OEtMe CN NHCOMe NC(O)C(O)NH2Me CN NHCOMe NC(O)C(O)OHMe CN NHCOMe NC(NH)NH2Me CN NHCOMe NC(NOH)NH2Me CN NHCOMe NC(NH)NHMeMe CN NHCOMe NC(NH)NMe2Me CN NHCOMe NC(NH)OMeMe CN NHCOMe NC(NH)OEtEt CN NHCOMe NCOMeEt CN NHCOMe NCOEtEt CN NHCOMe NCOPrEt CN NHCOMe NCHOEt CN NHCOMe NCOiPrEt CN NHCOMe NCOtBuEt CN NHCOMe NCOPhEt CN NHCOMe NSO2MeEt CN NHCOMe NSO2EtEt CN NHCOMe NSO2PrEt CN NHCOMe NSO2PhEt CN NHCOMe NSO2iPrEt CN NHCOMe NNO2Et CN NHCOMe NCOOMeEt CN NHCOMe NCOOEtEt CN NHCOMe NCOOPrEt CN NHCOMe NCOOiPrEt CN NHCOMe NCONHEtEt CN NHCOMe NCONHPrEt CN NHCOMe NCONH2Et CN NHCOMe NCONHMeEt CN NHCOMe NCNEt CN NHCOMe NCOSMeEt CN NHCOMe NCOSEt ¨Et CN NHCOMe NCSOMeEt CN NHCOMe NCSOEt ¨Et CN NHCOMe NCSOPrEt CN NHCOMe NSO2NH2Et CN NHCOMe NSO2NHMe ¨Et CN NHCOMe NSO2NMe2Et CN NHCOMe NP(O)(Ote)2Et CN NHCOMe NP(O)(OEt)2Et CN NHCOMe NP(O)Me2 ¨Et CN NHCOMe NP(O)Et2 ¨Et CN NHCOMe NP(O)Me(OMe) ¨Et CN NHCOMe NP(O)(OPr)2 ¨Et CN NHCOMe NC(O)C(O)H ¨Et CN NHCOMe NC(O)C(O)Me ¨Et CN NHCOMe NC(O)C(O)OMe ¨Et CN NHCOMe NC(O)C(O)OEtEt CN NHCOMe NC(O)C(O)NH2Et CN NHCOMe NC(O)C(O)OHEt CN NHCOMe NC(NH)NH2Et CN NHCOMe NC(NOH)NH2Et CN NHCOMe NC(NH)NHMeEt CN NHCOMe NC(NH)NMe2Et CN NHCOMe NC(NH)OMeEt CN NHCOMe NC(NH)OEtMe CN NHCOOMe NCOMeMe CN NHCOOMe NCOEtMe CN NHCOOMe NCOPrMe CN NHCOOMe NCHOMe CN NHCOOMe NCOiPrMe CN NHCOOMe NCOtBuMe CN NHCOOMe NCOPhMe CN NHCOOMe NSO2MeMe CN NHCOOMe NSO2EtMe CN NHCOOMe NSO2PrMe CN NHCOOMe NSO2PhMe CN NHCOOMe NSO2iPrMe CN NHCOOMe NNO2 ¨Me CN NHCOOMe NCOOMe ¨Me CN NHCOOMe NCOOEt ¨Me CN NHCOOMe NCOOPr ¨Me CN NHCOOMe NCOOiPr ¨Me CN NHCOOMe NCONHEt ¨Me CN NHCOOMe NCONHPr ¨Me CN NHCOOMe NCONH2 ¨Me CN NHCOOMe NCONHMe ¨Me CN NHCOOMe NCNMe CN NHCOOMe NCOSMeMe CN NHCOOMe NCOSEtMe CN NHCOOMe NCSOMeMe CN NHCOOMe NCSOEtMe CN NHCOOMe NCSOPrMe CN NHCOOMe NSO2NH2Me CN NHCOOMe NSO2NHMeMe CN NHCOOMe NSO2NMe2Me CN NHCOOMe NP(O)(OMe)2Me CN NHCOOMe NP(O)(OEt)2Me CN NHCOOMe NP(O)Me2Me CN NHCOOMe NP(O)Et2Me CN NHCOOMe NP(O)Me(OMe)Me CN NHCOOMe NP(O)(OPr)2Me CN NHCOOMe NC(O)C(O)HMe CN NHCOOMe NC(O)C(O)MeMe CN NHCOOMe NC(O)C(O)OMeMe CN NHCOOMe NC(O)C(O)OEtMe CN NHCOOMe NC(O)C(O)NH2 ¨Me CN NHCOOMe NC(O)C(O)OH ¨Me CN NHCOOMe NC(NH)NH2 ¨Me CN NHCOOMe NC(NOH)NH2 ¨Me CN NHCOOMe NC(NH)NHMe ¨Me CN NHCOOMe NC(NH)NMe2 ¨Me CN NHCOOMe NC(NH)OMe ¨Me CN NHCOOMe NC(NH)OEt ¨Et CN NHCOOMe NCOMe ¨Et CN NHCOOMe NCOEtEt CN NHCOOMe NCOPrEt CN NHCOOMe NCHOEt CN NHCOOMe NCOiPrEt CN NHCOOMe NCOtBuEt CN NHCOOMe NCOPhEt CN NHCOOMe NSO2MeEt CN NHCOOMe NSO2EtEt CN NHCOOMe NSO2PrEt CN NHCOOMe NSO2PhEt CN NHCOOMe NSO2iPrEt CN NHCOOMe NNO2 ¨Et CN NHCOOMe NCOOMe ¨Et CN NHCOOMe NCOOEtEt CN NHCOOMe NCOOPrEt CN NHCOOMe NCOOiPrEt CN NHCOOMe NCONHEtEt CN NHCOOMe NCONHPrEt CN NHCOOMe NCONH2Et CN NHCOOMe NCONHMeEt CN NHCOOMe NCN ¨Et CN NHCOOMe NCOSMe ¨Et CN NHCOOMe NCOSEt ¨Et CN NHCOOMe NCSOMe ¨Et CN NHCOOMe NCSOEt ¨Et CN NHCOOMe NCSOPr ¨Et CN NHCOOMe NSO2NH2 ¨Et CN NHCOOMe NSO2NHMeEt CN NHCOOMe NSO2NMe2Et CN NHCOOMe NP(O)(OMe)2Et CN NHCOOMe NP(O)(OEt)2Et CN NHCOOMe NP(O)Me2Et CN NHCOOMe NP(O)Et2Et CN NHCOOMe NP(O)Me(OMe)Et CN NHCOOMe NP(O)(OPr)2Et CN NHCOOMe NC(O)C(O)HEt CN NHCOOMe NC(O)C(O)MeEt CN NHCOOMe NC(O)C(O)OMeEt CN NHCOOMe NC(O)C(O)OEtEt CN NHCOOMe NC(O)C(O)NH2Et CN NHCOOMe NC(O)C(O)OHEt CN NHCOOMe NC(NH)NH2Et CN NHCOOMe NC(NOH)NH2Et CN NHCOOMe NC(NH)NHMeMe CN NHCOOEt NCSOEtMe CN NHCOOEt NCSOPrMe CN NHCOOEt NSO2NH2Me CN NHCOOEt NSO2NHMeMe CN NHCOOEt NSO2NMe2 ¨Me CN NHCOOEt NP(O)(OMe)2 ¨Me CN NHCOOEt NP(O)(OEt)2 ¨Me CN NHCOOEt NP(O)Me2 ¨Me CN NHCOOEt NP(O)Et2 ¨Me CN NHCOOEt NP(O)Me(OMe) ¨Me CN NHCOOEt NP(O)(OPr)2Me CN NHCOOEt NC(O)C(O)HMe CN NHCOOEt NC(O)C(O)MeMe CN NHCOOEt NC(O)C(O)OMeMe CN NHCOOEt NC(O)C(O)OEtMe CN NHCOOEt NC(O)C(O)NH2Me CN NHCOOEt NC(O)C(O)OHMe CN NHCOOEt NC(NH)NH2Me CN NHCOOEt NC(NOH)NH2Me CN NHCOOEt NC(NH)NHMeMe CN NHCOOEt NC(NH)NMe2Me CN NHCOOEt NC(NH)OMeMe CN NHCOOEt NC(NH)OEtEt CN NHCOOEt NCOMeEt CN NHCOOEt NCOEtEt CN NHCOOEt NCOPr ¨Et CN NHCOOEt NCHOEt CN NHCOOEt NCOiPrEt CN NHCOOMe NC(NH)NMe2Et CN NHCOOMe NC(NH)OMeEt CN NHCOOMe NC(NH)OEtMe CN NHCOOEt NCOMe ¨Me CN NHCOOEt NCOEtMe CN NHCOOEt NCOPr ¨Me CN NHCOOEt NCHO ¨Me CN NHCOOEt NCOiPr ¨Me CN NHCOOEt NCOtBu ¨Me CN NHCOOEt NCOPhMe CN NHCOOEt NSO2MeMe CN NHCOOEt NSO2EtMe CN NHCOOEt NSO2PrMe CN NHCOOEt NSO2PhMe CN NHCOOEt NSO2iPrMe CN NHCOOEt NNO2Me CN NHCOOEt NCOOMeMe CN NHCOOEt NCOOEtMe CN NHCOOEt NCOOPrMe CN NHCOOEt NCOOiPrMe CN NHCOOEt NCONHEtMe CN NHCOOEt NCONHPrMe CN NHCOOEt NCONH2Me CN NHCOOEt NCONHMeMe CN NHCOOEt NCNMe CN NHCOOEt NCOSMeMe CN NHCOOEt NCOSEtMe CN NHCOOEt NCSOMeEt CN NHCOOEt NCOtBuEt CN NHCOOEt NCOPhEt CN NHCOOEt NSO2MeEt CN NHCOOEt NSO2EtEt CN NHCOOEt NSO2PrEt CN NHCOOEt NSO2Ph ¨Et CN NHCOOEt NSO2iPr ¨Et CN NHCOOEt NNO2 ¨Et CN NHCOOEt NCOOMe ¨Et CN NHCOOEt NCOOEt ¨Et CN NHCOOEt NCOOPrEt CN NHCOOEt NCOOiPrEt CN NHCOOEt NCONHEtEt CN NHCOOEt NCONHPrEt CN NHCOOEt NCONH2Et CN NHCOOEt NCONHMeEt CN NHCOOEt NCNEt CN NHCOOEt NCOSMeEt CN NHCOOEt NCOSEtEt CN NHCOOEt NCSOMeEt CN NHCOOEt NCSOEtEt CN NHCOOEt NCSOPrEt CN NHCOOEt NSO2NH2Et CN NHCOOEt NSO2NHMeEt CN NHCOOEt NSO2NMe2Et CN NHCOOEt NP(O)(OMe)2Et CN NHCOOEt NP(O)(OEt)2Et CN NHCOOEt NP(O)Me2 ¨Et CN NHCOOEt NP(O)Et2Et CN NHCOOEt NP(O)Me(OMe)Et CN NHCOOEt NP(O)(OPr)2Et CN NHCOOEt NC(O)C(O)HEt CN NHCOOEt NC(O)C(O)MeEt CN NHCOOEt NC(O)C(O)OMe ¨Et CN NHCOOEt NC(O)C(O)OEt ¨Et CN NHCOOEt NC(O)C(O)NH2 ¨Et CN NHCOOEt NC(O)C(O)OH ¨Et CN NHCOOEt NC(NH)NH2 ¨Et CN NHCOOEt NC(NOH)NH2Et CN NHCOOEt NC(NH)NHMeEt CN NHCOOEt NC(NH)NMe2Et CN NHCOOEt NC(NH)OMeEt CN NHCOOEt NC(NH)OEtMe CN NHCH2COOMe NCOMeMe CN NHCH2COOMe NCOEtMe CN NHCH2COOMe NCOPrMe CN NHCH2COOMe NCHOMe CN NHCH2COOMe NCOiPrMe CN NHCH2COOMe NCOtBuMe CN NHCH2COOMe NCOPhMe CN NHCH2COOMe NSO2MeMe CN NHCH2COOMe NSO2EtMe CN NHCH2COOMe NSO2PrMe CN NHCH2COOMe NSO2PhMe CN NHCH2COOMe NSO2iPrMe CN NHCH2COOMe NNO2Me CN NHCH2COOMe NCOOMeMe CN NHCH2COOMe NCOOEtMe CN NHCH2COOMe NCOOPrMe CN NHCH2COOMe NCOOiPrMe CN NHCH2COOMe NCONHEtMe CN NHCH2COOMe NCONHPr ¨Me CN NHCH2COOMe NCONH2 ¨Me CN NHCH2COOMe NCONHMe ¨Me CN NHCH2COOMe NCN ¨Me CN NHCH2COOMe NCOSMe ¨Me CN NHCH2COOMe NCOSEtMe CN NHCH2COOMe NCSOMeMe CN NHCH2COOMe NCSOEtMe CN NHCH2COOMe NCSOPrMe CN NHCH2COOMe NSO2NH2Me CN NHCH2COOMe NSO2NHMeMe CN NHCH2COOMe NSO2NMe2Me CN NHCH2COOMe NP(O)(OMe)2Me CN NHCH2COOMe NP(O)(OEt)2Me CN NHCH2COOMe NP(O)Me2Me CN NHCH2COOMe NP(O)Et2Me CN NHCH2COOMe NP(O)Me(OMe)Me CN NHCH2COOMe NP(O)(OPr)2Me CN NHCH2COOMe NC(O)C(O)HMe CN NHCH2COOMe NC(O)C(O)MeMe CN NHCH2COOMe NC(O)C(O)OMeMe CN NHCH2COOMe NC(O)C(O)OEtMe CN NHCH2COOMe NC(O)C(O)NH2Me CN NHCH2COOMe NC(O)C(O)OHMe CN NHCH2COOMe NC(NH)NH2Me CN NHCH2COOMe NC(NOH)NH2Me CN NHCH2COOMe NC(NH)NHMeMe CN NHCH2COOMe NC(NH)NMe2 ¨Me CN NHCH2COOMe NC(NH)OMe ¨Me CN NHCH2COOMe NC(NH)OEt ¨Et CN NHCH2COOMe NCOMe ¨Et CN NHCH2COOMe NCOEtEt CN NHCH2COOMe NCOPrEt CN NHCH2COOMe NCHOEt CN NHCH2COOMe NCOiPrEt CN NHCH2COOMe NCOtBuEt CN NHCH2COOMe NCOPhEt CN NHCH2COOMe NSO2MeEt CN NHCH2COOMe NSO2EtEt CN NHCH2COOMe NSO2PrEt CN NHCH2COOMe NSO2PhEt CN NHCH2COOMe NSO2iPrEt CN NHCH2COOMe NNO2Et CN NHCH2COOMe NCOOMeEt CN NHCH2COOMe NCOOEtEt CN NHCH2COOMe NCOOPrEt CN NHCH2COOMe NCOOiPrEt CN NHCH2COOMe NCONHEtEt CN NHCH2COOMe NCONHPrEt CN NHCH2COOMe NCONH2Et CN NHCH2COOMe NCONHMeEt CN NHCH2COOMe NCNEt CN NHCH2COOMe NCOSMeEt CN NHCH2COOMe NCOSEtEt CN NHCH2COOMe NCSOMe ¨Et CN NHCH2COOMe NCSOEt ¨Et CN NHCH2COOMe NCSOPr ¨Et CN NHCH2COOMe NSO2NH2 ¨Et CN NHCH2COOMe NSO2NHMe ¨Et CN NHCH2COOMe NSO2NMe2 ¨Et CN NHCH2COOMe NP(O)(OMe)2Et CN NHCH2COOMe NP(O)(OEt)2Et CN NHCH2COOMe NP(O)Me2Et CN NHCH2COOMe NP(O)Et2Et CN NHCH2COOMe NP(O)Me(OMe)Et CN NHCH2COOMe NP(O)(OPr)2Et CN NHCH2COOMe NC(O)C(O)HEt CN NHCH2COOMe NC(O)C(O)MeEt CN NHCH2COOMe NC(O)C(O)OMeEt CN NHCH2COOMe NC(O)C(O)OEtEt CN NHCH2COOMe NC(O)C(O)NH2Et CN NHCH2COOMe NC(O)C(O)OHEt CN NHCH2COOMe NC(NH)NH2Et CN NHCH2COOMe NC(NOH)NH2Et CN NHCH2COOMe NC(NH)NHMeEt CN NHCH2COOMe NC(NH)NMe2Et CN NHCH2COOMe NC(NH)OMeEt CN NHCH2COOMe NC(NH)OEtMe CN NHCH2CN NCOMeMe CN NHCH2CN NCOEtMe CN NHCH2CN NCOPrMe CN NHCH2CN NCHOMe CN NHCH2CN NCOiPrMe CN NHCH2CN NCOtBuMe CN NHCH2CN NCOPhMe CN NHCH2CN NSO2Me ¨Me CN NHCH2CN NSO2Et ¨Me CN NHCH2CN NSO2PrMe CN NHCH2CN NSO2PhMe CN NHCH2CN NSO2iPrMe CN NHCH2CN NNO2Me CN NHCH2CN NCOOMeMe CN NHCH2CN NCOOEtMe CN NHCH2CN NCOOPrMe CN NHCH2CN NCOOiPrMe CN NHCH2CN NCONHEtMe CN NHCH2CN NCONHPrMe CN NHCH2CN NCONH2Me CN NHCH2CN NCONHMeMe CN NHCH2CN NCNMe CN NHCH2CN NCOSMeMe CN NHCH2CN NCOSEtMe CN NHCH2CN NCSOMeMe CN NHCH2CN NCSOEtMe CN NHCH2CN NCSOPrMe CN NHCH2CN NSO2NH2Me CN NHCH2CN NSO2NHMeMe CN NHCH2CN NSO2NMe2Me CN NHCH2CN NP(O)(OMe)2Me CN NHCH2CN NP(O)(OEt)2Me CN NHCH2CN NP(O)Me2 ¨Me CN NHCH2CN NP(O)Et2Me CN NHCH2CN NP(O)Me(OMe) ¨Me CN NHCH2CN NP(O)(OPr)2 ¨Me CN NHCH2CN NC(O)C(O)H ¨Me CN NHCH2CN NC(O)C(O)Me ¨Me CN NHCH2CN NC(O)C(O)OMe ¨Me CN NHCH2CN NC(O)C(O)OEtMe CN NHCH2CN NC(O)C(O)NH2Me CN NHCH2CN NC(O)C(O)OHMe CN NHCH2CN NC(NH)NH2Me CN NHCH2CN NC(NOH)NH2Me CN NHCH2CN NC(NH)NHMeMe CN NHCH2CN NC(NH)NMe2Me CN NHCH2CN NC(NH)OMeMe CN NHCH2CN NC(NH)OEtEt CN NHCH2CN NCOMeEt CN NHCH2CN NCOEtEt CN NHCH2CN NCOPrEt CN NHCH2CN NCHOEt CN NHCH2CN NCOiPrEt CN NHCH2CN NCOtBuEt CN NHCH2CN NCOPhEt CN NHCH2CN NSO2MeEt CN NHCH2CN NSO2EtEt CN NHCH2CN NSO2PrEt CN NHCH2CN NSO2PhEt CN NHCH2CN NSO2iPr ¨Et CN NHCH2CN NNO2 ¨Et CN NHCH2CN NCOOMe ¨Et CN NHCH2CN NCOOEt ¨Et CN NHCH2CN NCOOPr ¨Et CN NHCH2CN NCOOiPr ¨Et CN NHCH2CN NCONHEt ¨Et CN NHCH2CN NCONHPr ¨Et CN NHCH2CN NCONH2 ¨Et CN NHCH2CN NCONHMeEt CN NHCH2CN NCNEt CN NHCH2CN NCOSMeEt CN NHCH2CN NCOSEtEt CN NHCH2CN NCSOMeEt CN NHCH2CN NCSOEtEt CN NHCH2CN NCSOPrEt CN NHCH2CN NSO2NH2Et CN NHCH2CN NSO2NHMeEt CN NHCH2CN NSO2NMe2Et CN NHCH2CN NP(O)(OMe)2Et CN NHCH2CN NP(O)(OEt)2Et CN NHCH2CN NP(O)Me2Et CN NHCH2CN NP(O)Et2Et CN NHCH2CN NP(O)Me(OMe)Et CN NHCH2CN NP(O)(OPr)2Et CN NHCH2CN NC(O)C(O)HEt CN NHCH2CN NC(O)C(O)MeEt CN NHCH2CN NC(O)C(O)OMeEt CN NHCH2CN NC(O)C(O)OEt ¨Et CN NHCH2CN NC(O)C(O)NH2 ¨Et CN NHCH2CN NC(O)C(O)OH ¨Et CN NHCH2CN NC(NH)NH2 ¨Et CN NHCH2CN NC(NOH)NH2 ¨Et CN NHCH2CN NC(NH)NHMe ¨Et CN NHCH2CN NC(NH)NMe2 ¨Et CN NHCH2CN NC(NH)OMe ¨Et CN NHCH2CN NC(NH)OEtMe CN NHCH2CONH2 NCOMeMe CN NHCH2CONH2 NCOEtMe CN NHCH2CONH2 NCOPrMe CN NHCH2CONH2 NCHOMe CN NHCH2CONH2 NCOiPrMe CN NHCH2CONH2 NCOtBuMe CN NHCH2CONH2 NCOPhMe CN NHCH2CONH2 NSO2MeMe CN NHCH2CONH2 NSO2EtMe CN NHCH2CONH2 NSO2PrMe CN NHCH2CONH2 NSO2Ph ¨Me CN NHCH2CONH2 NSO2iPrMe CN NHCH2CONH2 NNO2Me CN NHCH2CONH2 NCOOMeMe CN NHCH2CONH2 NCOOEtMe CN NHCH2CONH2 NCOOPr ¨Me CN NHCH2CONH2 NCOOiPr ¨Me CN NHCH2CONH2 NCONHEtMe CN NHCH2CONH2 NCONHPrMe CN NHCH2CONH2 NCONH2Me CN NHCH2CONH2 NCONHMeMe CN NHCH2CONH2 NCN ¨Me CN NHCH2CONH2 NCOSMe ¨Me CN NHCH2CONH2 NCOSEt ¨Me CN NHCH2CONH2 NCSOMe ¨Me CN NHCH2CONH2 NCSOEt ¨Me CN NHCH2CONH2 NCSOPrMe CN NHCH2CONH2 NSO2NH2Me CN NHCH2CONH2 NSO2NHMeMe CN NHCH2CONH2 NSO2NMe2Me CN NHCH2CONH2 NP(O)(OMe)2Me CN NHCH2CONH2 NP(O)(OEt)2Me CN NHCH2CONH2 NP(O)Me2Me CN NHCH2CONH2 NP(O)Et2Me CN NHCH2CONH2 NP(O)Me(OMe)Me CN NHCH2CONH2 NP(O)(OPr)2Me CN NHCH2CONH2 NC(O)C(O)HMe CN NHCH2CONH2 NC(O)C(O)MeMe CN NHCH2CONH2 NC(O)C(O)OMeMe CN NHCH2CONH2 NC(O)C(O)OEtMe CN NHCH2CONH2 NC(O)C(O)NH2 ¨Me CN NHCH2CONH2 NC(O)C(O)OH ¨Me CN NHCH2CONH2 NC(NH)NH2Me CN NHCH2CONH2 NC(NOH)NH2Me CN NHCH2CONH2 NC(NH)NHMeMe CN NHCH2CONH2 NC(NH)NMe2Me CN NHCH2CONH2 NC(NH)OMeMe CN NHCH2CONH2 NC(NH)OEtEt CN NHCH2CONH2 NCOMe ¨Et CN NHCH2CONH2 NCOEt ¨Et CN NHCH2CONH2 NCOPr ¨Et CN NHCH2CONH2 NCHO ¨Et CN NHCH2CONH2 NCOiPr ¨Et CN NHCH2CONH2 NCOtBu ¨Et CN NHCH2CONH2 NCOPh ¨Et CN NHCH2CONH2 NSO2Me ¨Et CN NHCH2CONH2 NSO2Et ¨Et CN NHCH2CONH2 NSO2PrEt CN NHCH2CONH2 NSO2PhEt CN NHCH2CONH2 NSO2iPrEt CN NHCH2CONH2 NNO2Et CN NHCH2CONH2 NCOOMeEt CN NHCH2CONH2 NCOOEtEt CN NHCH2CONH2 NCOOPrEt CN NHCH2CONH2 NCOOiPrEt CN NHCH2CONH2 NCONHEtEt CN NHCH2CONH2 NCONHPrEt CN NHCH2CONH2 NCONH2Et CN NHCH2CONH2 NCONHMeEt CN NHCH2CONH2 NCNEt CN NHCH2CONH2 NCOSMeEt CN NHCH2CONH2 NCOSEtEt CN NHCH2CONH2 NCSOMeEt CN NHCH2CONH2 NCSOEtEt CN NHCH2CONH2 NCSOPrEt CN NHCH2CONH2 NSO2NH2 ¨Et CN NHCH2CONH2 NSO2NHMe ¨Et CN NHCH2CONH2 NSO2NMe2 ¨Et CN NHCH2CONH2 NP(O)(OMe)2 ¨Et CN NHCH2CONH2 NP(O)(OEt)2 ¨Et CN NHCH2CONH2 NP(O)Me2 ¨Et CN NHCH2CONH2 NP(O)Et2 ¨Et CN NHCH2CONH2 NP(O)Me(OMe) ¨Et CN NHCH2CONH2 NP(O)(OPr)2Et CN NHCH2CONH2 NC(O)C(O)HEt CN NHCH2CONH2 NC(O)C(O)MeEt CN NHCH2CONH2 NC(O)C(O)OMeEt CN NHCH2CONH2 NC(O)C(O)OEtEt CN NHCH2CONH2 NC(O)C(O)NH2Et CN NHCH2CONH2 NC(O)C(O)OHEt CN NHCH2CONH2 NC(NH)NH2Et CN NHCH2CONH2 NC(NOH)NH2Et CN NHCH2CONH2 NC(NH)NHMeEt CN NHCH2CONH2 NC(NH)NMe2Et CN NHCH2CONH2 NC(NH)OMeEt CN NHCH2CONH2 NC(NH)OEtMe CN NHCH2CH2SMe NCOMeMe CN NHCH2CH2SMe NCOEtMe CN NHCH2CH2SMe NCOPrMe CN NHCH2CH2SMe NCHOMe CN NHCH2CH2SMe NCOiPrMe CN NHCH2CH2SMe NCOtBuMe CN NHCH2CH2SMe NCOPhMe CN NHCH2CH2SMe NSO2Me ¨Me CN NHCH2CH2SMe NSO2Et ¨Me CN NHCH2CH2SMe NSO2Pr ¨Me CN NHCH2CH2SMe NSO2Ph ¨Me CN NHCH2CH2SMe NSO2iPr ¨Me CN NHCH2CH2SMe NNO2 ¨Me CN NHCH2CH2SMe NCOOMe ¨Me CN NHCH2CH2SMe NCOOEt ¨Me CN NHCH2CH2SMe NCOOPrMe CN NHCH2CH2SMe NCOOiPrMe CN NHCH2CH2SMe NCONHEtMe CN NHCH2CH2SMe NCONHPrMe CN NHCH2CH2SMe NCONH2Me CN NHCH2CH2SMe NCONHMeMe CN NHCH2CH2SMe NCNMe CN NHCH2CH2SMe NCOSMeMe CN NHCH2CH2SMe NCOSEtMe CN NHCH2CH2SMe NCSOMeMe CN NHCH2CH2SMe NCSOEtMe CN NHCH2CH2SMe NCSOPrMe CN NHCH2CH2SMe NSO2NH2Me CN NHCH2CH2SMe NSO2NHMeMe CN NHCH2CH2SMe NSO2NMe2Me CN NHCH2CH2SMe NP(O)(OMe)2Me CN NHCH2CH2SMe NP(O)(OEt)2Me CN NHCH2CH2SMe NP(O)Me2Me CN NHCH2CH2SMe NP(O)Et2Me CN NHCH2CH2SMe NP(O)Me(OMe) ¨Me CN NHCH2CH2SMe NP(O)(OPr)2 ¨Me CN NHCH2CH2SMe NC(O)C(O)H ¨Me CN NHCH2CH2SMe NC(O)C(O)Me ¨Me CN NHCH2CH2SMe NC(O)C(O)OMe ¨Me CN NHCH2CH2SMe NC(O)C(O)OEt ¨Me CN NHCH2CH2SMe NC(O)C(O)NH2 ¨Me CN NHCH2CH2SMe NC(O)C(O)OH ¨Me CN NHCH2CH2SMe NC(NH)NH2 ¨Me CN NHCH2CH2SMe NC(NOH)NH2 ¨Me CN NHCH2CH2SMe NC(NH)NHMeMe CN NHCH2CH2SMe NC(NH)NMe2Me CN NHCH2CH2SMe NC(NH)OMeMe CN NHCH2CH2SMe NC(NH)OEtMe CN NHCH2CH2SOMe NCOMeMe CN NHCH2CH2SOMe NCOEtMe CN NHCH2CH2SOMe NCOPrMe CN NHCH2CH2SOMe NCHOMe CN NHCH2CH2SOMe NCOiPrMe CN NHCH2CH2SOMe NCOtBuMe CN NHCH2CH2SOMe NCOPh ¨Me CN NHCH2CH2SOMe NSO2MeMe CN NHCH2CH2SOMe NSO2EtMe CN NHCH2CH2SOMe NSO2PrMe CN NHCH2CH2SOMe NSO2Ph ¨Me CN NHCH2CH2SOMe NSO2iPrMe CN NHCH2CH2SOMe NNO2Me CN NHCH2CH2SOMe NCOOMeMe CN NHCH2CH2SOMe NCOOEtMe CN NHCH2CH2SOMe NCOOPrMe CN NHCH2CH2SOMe NCOOiPr ¨Me CN NHCH2CH2SOMe NCONHEt ¨Me CN NHCH2CH2SOMe NCONHPr ¨Me CN NHCH2CH2SOMe NCONH2 ¨Me CN NHCH2CH2SOMe NCONHMe ¨Me CN NHCH2CH2SOMe NCN ¨Me CN NHCH2CH2SOMe NCOSMe ¨Me CN NHCH2CH2SOMe NCOSEtMe CN NHCH2CH2SOMe NCSOMeMe CN NHCH2CH2SOMe NCSOEtMe CN NHCH2CH2SOMe NCSOPrMe CN NHCH2CH2SOMe NSO2NH2Me CN NHCH2CH2SOMe NSO2NHMeMe CN NHCH2CH2SOMe NSO2NMe2Me CN NHCH2CH2SOMe NP(O)(OMe)2Me CN NHCH2CH2SOMe NP(O)(OEt)2Me CN NHCH2CH2SOMe NP(O)Me2Me CN NHCH2CH2SOMe NP(O)Et2Me CN NHCH2CH2SOMe NP(O)Me(OMe)Me CN NHCH2CH2SOMe NP(O)(OPr)2Me CN NHCH2CH2SOMe NC(O)C(O)HMe CN NHCH2CH2SOMe NC(O)C(O)MeMe CN NHCH2CH2SOMe NC(O)C(O)OMeMe CN NHCH2CH2SOMe NC(O)C(O)OEtMe CN NHCH2CH2SOMe NC(O)C(O)NH2Me CN NHCH2CH2SOMe NC(O)C(O)OHMe CN NHCH2CH2SOMe NC(NH)NH2Me CN NHCH2CH2SOMe NC(NOH)NH2Me CN NHCH2CH2SOMe NC(NH)NHMe ¨Me CN NHCH2CH2SOMe NC(NH)NMe2 ¨Me CN NHCH2CH2SOMe NC(NH)OMe ¨Me CN NHCH2CH2SOMe NC(NH)OEt ¨Et CN NHCH2CH2SMe NCOMe ¨Et CN NHCH2CH2SMe NCOEt ¨Et CN NHCH2CH2SMe NCOPr ¨Et CN NHCH2CH2SMe NCHO ¨Et CN NHCH2CH2SMe NCOiPrEt CN NHCH2CH2SMe NCOtBuEt CN NHCH2CH2SMe NCOPhEt CN NHCH2CH2SMe NSO2MeEt CN NHCH2CH2SMe NSO2EtEt CN NHCH2CH2SMe NSO2PrEt CN NHCH2CH2SMe NSO2PhEt CN NHCH2CH2SMe NSO2iPrEt CN NHCH2CH2SMe NNO2Et CN NHCH2CH2SMe NCOOMeEt CN NHCH2CH2SMe NCOOEtEt CN NHCH2CH2SMe NCOOPrEt CN NHCH2CH2SMe NCOOiPrEt CN NHCH2CH2SMe NCONHEtEt CN NHCH2CH2SMe NCONHPrEt CN NHCH2CH2SMe NCONH2Et CN NHCH2CH2SMe NCONHMeEt CN NHCH2CH2SMe NCNEt CN NHCH2CH2SMe NCOSMeEt CN NHCH2CH2SMe NCOSEtEt CN NHCH2CH2SMe NCSOMeEt CN NHCH2CH2SMe NCSOEtEt CN NHCH2CH2SMe NCSOPrEt CN NHCH2CH2SMe NSO2NH2Et CN NHCH2CH2SMe NSO2NHMeEt CN NHCH2CH2SMe NSO2NMe2Et CN NHCH2CH2SMe NP(O)(OMe)2Et CN NHCH2CH2SMe NP(O)(OEt)2Et CN NHCH2CH2SMe NP(O)Me2Et CN NHCH2CH2SMe NP(O)Et2Et CN NHCH2CH2SMe NP(O)Me(OMe)Et CN NHCH2CH2SMe NP(O)(OPr)2Et CN NHCH2CH2SMe NC(O)C(O)HEt CN NHCH2CH2SMe NC(O)C(O)MeEt CN NHCH2CH2SMe NC(O)C(O)OMeEt CN NHCH2CH2SMe NC(O)C(O)OEtEt CN NHCH2CH2SMe NC(O)C(O)NH2Et CN NHCH2CH2SMe NC(O)C(O)OHEt CN NHCH2CH2SMe NC(NH)NH2Et CN NHCH2CH2SMe NC(NOH)NH2Et CN NHCH2CH2SMe NC(NH)NHMeEt CN NHCH2CH2SMe NC(NH)NMe2Et CN NHCH2CH2SMe NC(NH)OMeEt CN NHCH2CH2SMe NC(NH)OEtEt CN NHCH2CH2SOMe NCOMeEt CN NHCH2CH2SOMe NCOEtEt CN NHCH2CH2SOMe NCOPr ¨Et CN NHCH2CH2SOMe NCHO ¨Et CN NHCH2CH2SOMe NCOiPr ¨Et CN NHCH2CH2SOMe NCOtBu ¨Et CN NHCH2CH2SOMe NCOPh ¨Et CN NHCH2CH2SOMe NSO2Me ¨Et CN NHCH2CH2SOMe NSO2Et ¨Et CN NHCH2CH2SOMe NSO2Pr ¨Et CN NHCH2CH2SOMe NSO2Ph ¨Et CN NHCH2CH2SOMe NSO2iPrEt CN NHCH2CH2SOMe NNO2Et CN NHCH2CH2SOMe NCOOMeEt CN NHCH2CH2SOMe NCOOEtEt CN NHCH2CH2SOMe NCOOPrEt CN NHCH2CH2SOMe NCOOiPrEt CN NHCH2CH2SOMe NCONHEtEt CN NHCH2CH2SOMe NCONHPrEt CN NHCH2CH2SOMe NCONH2Et CN NHCH2CH2SOMe NCONHMeEt CN NHCH2CH2SOMe NCNEt CN NHCH2CH2SOMe NCOSMeEt CN NHCH2CH2SOMe NCOSEtEt CN NHCH2CH2SOMe NCSOMeEt CN NHCH2CH2SOMe NCSOEtEt CN NHCH2CH2SOMe NCSOPrEt CN NHCH2CH2SOMe NSO2NH2Et CN NHCH2CH2SOMe NSO2NHMeEt CN NHCH2CH2SOMe NSO2NMe2Et CN NHCH2CH2SOMe NP(O)(OMe)2Et CN NHCH2CH2SOMe NP(O)(OEt)2Et CN NHCH2CH2SOMe NP(O)Me2Et CN NHCH2CH2SOMe NP(O)Et2Et CN NHCH2CH2SOMe NP(O)Me(OMe)Et CN NHCH2CH2SOMe NP(O)(OPr)2Et CN NHCH2CH2SOMe NC(O)C(O)HEt CN NHCH2CH2SOMe NC(O)C(O)MeEt CN NHCH2CH2SOMe NC(O)C(O)OMeEt CN NHCH2CH2SOMe NC(O)C(O)OEtEt CN NHCH2CH2SOMe NC(O)C(O)NH2Et CN NHCH2CH2SOMe NC(O)C(O)OHEt CN NHCH2CH2SOMe NC(NH)NH2Et CN NHCH2CH2SOMe NC(NOH)NH2Et CN NHCH2CH2SOMe NC(NH)NHMeEt CN NHCH2CH2SOMe NC(NH)NMe2Et CN NHCH2CH2SOMe NC(NH)OMeEt CN NHCH2CH2SOMe NC(NH)OEtMe CN NHCOMe NCOMe OMe CN NHCOMe NCOEt OMe CN NHCOMe NCOPr OMe CN NHCOMe NCHO OMe CN NHCOMe NCOiPr OMe CN NHCOMe NCOtBu OMe CN NHCOMe NCOPh OMe CN NHCOMe NSO2Me OMe CN NHCOMe NSO2Et OMe CN NHCOMe NSO2Pr OMe CN NHCOMe NSO2Ph OMe CN NHCOMe NSO2iPr OMe CN NHCOMe NNO2 OMe CN NHCOMe NCOOMe OMe CN NHCOMe NCOOEt OMe CN NHCOMe NCOOPr OMe CN NHCOMe NCOOiPr OMe CN NHCOMe NCONHEt OMe CN NHCOMe NCONHPr OMe CN NHCOMe NCONH2 OMe CN NHCOMe NCONHMe OMe CN NHCOMe NCN OMe CN NHCOMe NCOSMe OMe CN NHCOMe NCOSEt OMe CN NHCOMe NCSOMe OMe CN NHCOMe NCSOEt OMe CN NHCOMe NCSOPr OMe CN NHCOMe NSO2NH2 OMe CN NHCOMe NSO2NHMe OMe CN NHCOMe NSO2NMe2 OMe CN NHCOMe NP(O)(OMe)2 OMe CN NHCOMe NP(O)(OEt)2 OMe CN NHCOMe NP(O)Me2 OMe CN NHCOMe NP(O)Et2 OMe CN NHCOMe NP(O)Me(OMe) OMe CN NHCOMe NP(O)(OPr)2 OMe CN NHCOMe NC(O)C(O)H OMe CN NHCOMe NC(O)C(O)Me OMe CN NHCOMe NC(O)C(O)OMe OMe CN NHCOMe NC(O)C(O)OEt OMe CN NHCOMe NC(O)C(O)NH2 OMe CN NHCOMe NC(O)C(O)OH OMe CN NHCOMe NC(NH)NH2 OMe CN NHCOMe NC(NOH)NH2 OMe CN NHCOMe NC(NH)NHMe OMe CN NHCOMe NC(NH)NMe2 OMe CN NHCOMe NC(NH)OMe OMe CN NHCOMe NC(NH)OEt OEt CN NHCOMe NCOMe OEt CN NHCOMe NCOEt OEt CN NHCOMe NCOPr OEt CN NHCOMe NCHO OEt CN NHCOMe NCOiPr OEt CN NHCOMe NCOtBu OEt CN NHCOMe NCOPh OEt CN NHCOMe NSO2Me OEt CN NHCOMe NSO2Et OEt CN NHCOMe NSO2Pr OEt CN NHCOMe NSO2Ph OEt CN NHCOMe NSO2iPr OEt CN NHCOMe NNO2 OEt CN NHCOMe NCOOMe OEt CN NHCOMe NCOOEt OEt CN NHCOMe NCOOPr OEt CN NHCOMe NCOOiPr OEt CN NHCOMe NCONHEt OEt CN NHCOMe NCONHPr OEt CN NHCOMe NCONH2 OEt CN NHCOMe NCONHMe OEt CN NHCOMe NCN OEt CN NHCOMe NCOSMe OEt CN NHCOMe NCOSEt OEt CN NHCOMe NCSOMe OEt CN NHCOMe NCSOEt OEt CN NHCOMe NCSOPr OEt CN NHCOMe NSO2NH2 OEt CN NHCOMe NSO2NHMe OEt CN NHCOMe NSO2NMe2 OEt CN NHCOMe NP(O)(OMe)2 OEt CN NHCOMe NP(O)(OEt)2 OEt CN NHCOMe NP(O)Me2 OEt CN NHCOMe NP(O)Et2 OEt CN NHCOMe NP(O)Me(OMe) OEt CN NHCOMe NP(O)(OPr)2 OEt CN NHCOMe NC(O)C(O)H OEt CN NHCOMe NC(O)C(O)Me OEt CN NHCOMe NC(O)C(O)OMe OEt CN NHCOMe NC(O)C(O)OEt OEt CN NHCOMe NC(O)C(O)NH2 OEt CN NHCOMe NC(O)C(O)OH OEt CN NHCOMe NC(NH)NH2 OEt CN NHCOMe NC(NOH)NH2 OEt CN NHCOMe NC(NH)NHMe OEt CN NHCOMe NC(NH)NMe2 OEt CN NHCOMe NC(NH)OMe OEt CN NHCOMe NC(NH)OEt OMe CN NHCOOMe NCOMe OMe CN NHCOOMe NCOEt OMe CN NHCOOMe NCOPr OMe CN NHCOOMe NCHO OMe CN NHCOOMe NCOiPr OMe CN NHCOOMe NCOtBu OMe CN NHCOOMe NCOPh OMe CN NHCOOMe NSO2Me OMe CN NHCOOMe NSO2Et OMe CN NHCOOMe NSO2Pr OMe CN NHCOOMe NSO2Ph OMe CN NHCOOMe NSO2iPr OMe CN NHCOOMe NNO2 OMe CN NHCOOMe NCOOMe OMe CN NHCOOMe NCOOEt OMe CN NHCOOMe NCOOPr OMe CN NHCOOMe NCOOiPr OMe CN NHCOOMe NCONHEt OMe CN NHCOOMe NCONHPr OMe CN NHCOOMe NCONH2 OMe CN NHCOOMe NCONHMe OMe CN NHCOOMe NCN OMe CN NHCOOMe NCOSMe OMe CN NHCOOMe NCOSEt OMe CN NHCOOMe NCSOMe OMe CN NHCOOMe NCSOEt OMe CN NHCOOMe NCSOPr OMe CN NHCOOMe NSO2NH2 OMe CN NHCOOMe NSO2NHMe OMe CN NHCOOMe NSO2NMe2 OMe CN NHCOOMe NP(O)(OMe)2 OMe CN NHCOOMe NP(O)(OEt)2 OMe CN NHCOOMe NP(O)Me2 OMe CN NHCOOMe NP(O)Et2 OMe CN NHCOOMe NP(O)Me(OMe) OMe CN NHCOOMe NP(O)(OPr)2 OMe CN NHCOOMe NC(O)C(O)H OMe CN NHCOOMe NC(O)C(O)Me OMe CN NHCOOMe NC(O)C(O)OMe OMe CN NHCOOMe NC(O)C(O)OEt OMe CN NHCOOMe NC(O)C(O)NH2 OMe CN NHCOOMe NC(O)C(O)OH OMe CN NHCOOMe NC(NH)NH2 OMe CN NHCOOMe NC(NOH)NH2 OMe CN NHCOOMe NC(NH)NHMe OMe CN NHCOOMe NC(NH)NMe2 OMe CN NHCOOMe NC(NH)OMe OMe CN NHCOOMe NC(NH)OEt OEt CN NHCOOMe NCOMe OEt CN NHCOOMe NCOEt OEt CN NHCOOMe NCOPr OEt CN NHCOOMe NCHO OEt CN NHCOOMe NCOiPr OEt CN NHCOOMe NCOtBu OEt CN NHCOOMe NCOPh OEt CN NHCOOMe NSO2Me OEt CN NHCOOMe NSO2Et OEt CN NHCOOMe NSO2Pr OEt CN NHCOOMe NSO2Ph OEt CN NHCOOMe NSO2iPr OEt CN NHCOOMe NNO2 OEt CN NHCOOMe NCOOMe OEt CN NHCOOMe NCOOEt OEt CN NHCOOMe NCOOPr OEt CN NHCOOMe NCOOiPr OEt CN NHCOOMe NCONHEt OEt CN NHCOOMe NCONHPr OEt CN NHCOOMe NCONH2 OEt CN NHCOOMe NCONHMe OEt CN NHCOOMe NCN OEt CN NHCOOMe NCOSMe OEt CN NHCOOMe NCOSEt OEt CN NHCOOMe NCSOMe OEt CN NHCOOMe NCSOEt OEt CN NHCOOMe NCSOPr OEt CN NHCOOMe NSO2NH2 OEt CN NHCOOMe NSO2NHMe OEt CN NHCOOMe NSO2NMe2 OEt CN NHCOOMe NP(O)(OMe)2 OEt CN NHCOOMe NP(O)(OEt)2 OEt CN NHCOOMe NP(O)Me2 OEt CN NHCOOMe NP(O)Et2 OEt CN NHCOOMe NP(O)Me(OMe) OEt CN NHCOOMe NP(O)(OPr)2 OEt CN NHCOOMe NC(O)C(O)H OEt CN NHCOOMe NC(O)C(O)Me OEt CN NHCOOMe NC(O)C(O)OMe OEt CN NHCOOMe NC(O)C(O)OEt OEt CN NHCOOMe NC(O)C(O)NH2 OEt CN NHCOOMe NC(O)C(O)OH OEt CN NHCOOMe NC(NH)NH2 OEt CN NHCOOMe NC(NOH)NH2 OEt CN NHCOOMe NC(NH)NHMe OEt CN NHCOOMe NC(NH)NMe2 OEt CN NHCOOMe NC(NH)OMe OEt CN NHCOOMe NC(NH)OEt OCF3 CN NH2 NCOMeCF3 CN NH2 NCOEtCF3 CN NH2 NCOPrCF3 CN NH2 NCHOCF3 CN NH2 NCOiPrCF3 CN NH2 NCOtBuCF3 CN NH2 NCOPhCF3 CN NH2 NSO2MeCF3 CN NH2 NSO2EtCF3 CN NH2 NSO2PrCF3 CN NH2 NSO2PhCF3 CN NH2 NSO2iPrCF3 CN NH2 NNO2CF3 CN NH2 NCOOMeCF3 CN NH2 NCOOEt ¨CF3 CN NH2 NCOOPr ¨CF3 CN NH2 NCOOiPr ¨CF3 CN NH2 NCONHEt ¨CF3 CN NH2 NCONHPr ¨CF3 CN NH2 NCONH2 ¨CF3 CN NH2 NCONHMe ¨CF3 CN NH2 NCN ¨CF3 CN NH2 NCOSMe ¨CF3 CN NH2 NCOSEtCF3 CN NH2 NCSOMeCF3 CN NH2 NCSOEtCF3 CN NH2 NCSOPrCF3 CN NH2 NSO2NH2CF3 CN NH2 NSO2NHMeCF3 CN NH2 NSO2NMe2CF3 CN NH2 NP(O)(OMe)2CF3 CN NH2 NP(O)(OEt)2CF3 CN NH2 NP(O)Me2CF3 CN NH2 NP(O)Et2CF3 CN NH2 NP(O)Me(OMe)CF3 CN NH2 NP(O)(OPr)2CF3 CN NH2 NC(O)C(O)HCF3 CN NH2 NC(O)C(O)MeCF3 CN NH2 NC(O)C(O)OMeCF3 CN NH2 NC(O)C(O)OEtCF3 CN NH2 NC(O)C(O)NH2CF3 CN NH2 NC(O)C(O)OHCF3 CN NH2 NC(NH)NH2 ¨CF3 CN NH2 NC(NOH)NH2 ¨CF3 CN NH2 NC(NH)NHMe ¨CF3 CN NH2 NC(NH)NMe2 ¨CF3 CN NH2 NC(NH)OMe ¨CF3 CN NH2 NC(NH)OEt ¨CF3 CN NHMe NCOMe ¨CF3 CN NHMe NCOEt ¨CF3 CN NHMe NCOPr ¨CF3 CN NHMe NCHO ¨CF3 CN NHMe NCOiPrCF3 CN NHMe NCOtBuCF3 CN NHMe NCOPhCF3 CN NHMe NSO2MeCF3 CN NHMe NSO2EtCF3 CN NHMe NSO2PrCF3 CN NHMe NSO2PhCF3 CN NHMe NSO2iPrCF3 CN NHMe NNO2CF3 CN NHMe NCOOMe ¨CF3 CN NHMe NCOOEt ¨CF3 CN NHMe NCOOPrCF3 CN NHMe NCOOiPrCF3 CN NHMe NCONHEtCF3 CN NHMe NCONHPrCF3 CN NHMe NCONH2CF3 CN NHMe NCONHMeCF3 CN NHMe NCNCF3 CN NHMe NCOSMe ¨CF3 CN NHMe NCOSEt ¨CF3 CN NHMe NCSOMe ¨CF3 CN NHMe NCSOEt ¨CF3 CN NHMe NCSOPr ¨CF3 CN NHMe NSO2NH2 ¨CF3 CN NHMe NSO2NHMe ¨CF3 CN NHMe NSO2NMe2 ¨CF3 CN NHMe NP(O)(OMe)2 ¨CF3 CN NHMe NP(O)(OEt)2 ¨CF3 CN NHMe NP(O)Me2CF3 CN NHMe NP(O)Et2CF3 CN NHMe NP(O)Me(OMe)CF3 CN NHMe NP(O)(OPr)2CF3 CN NHMe NC(O)C(O)HCF3 CN NHMe NC(O)C(O)MeCF3 CN NHMe NC(O)C(O)OMeCF3 CN NHMe NC(O)C(O)OEtCF3 CN NHMe NC(O)C(O)NH2CF3 CN NHMe NC(O)C(O)OHCF3 CN NHMe NC(NH)NH2CF3 CN NHMe NC(NOH)NH2CF3 CN NHMe NC(NH)NHMeCF3 CN NHMe NC(NH)NMe2CF3 CN NHMe NC(NH)OMeCF3 CN NHMe NC(NH)OEtCF3 CN NHEt NCOMeCF3 CN NHEt NCOEtCF3 CN NHEt NCOPrCF3 CN NHEt NCHOCF3 CN NHEt NCOiPr ¨CF3 CN NHEt NCOtBu ¨CF3 CN NHEt NCOPh ¨CF3 CN NHEt NSO2Me ¨CF3 CN NHEt NSO2Et ¨CF3 CN NHEt NSO2Pr ¨CF3 CN NHEt NSO2Ph ¨CF3 CN NHEt NSO2iPrCF3 CN NHEt NNO2CF3 CN NHEt NCOOMeCF3 CN NHEt NCOOEtCF3 CN NHEt NCOOPrCF3 CN NHEt NCOOiPrCF3 CN NHEt NCONHEtCF3 CN NHEt NCONHPrCF3 CN NHEt NCONH2CF3 CN NHEt NCONHMeCF3 CN NHEt NCNCF3 CN NHEt NCOSMeCF3 CN NHEt NCOSEtCF3 CN NHEt NCSOMeCF3 CN NHEt NCSOEtCF3 CN NHEt NCSOPrCF3 CN NHEt NSO2NH2CF3 CN NHEt NSO2NHMeCF3 CN NHEt NSO2NMe2CF3 CN NHEt NP(O)(OMe)2CF3 CN NHEt NP(O)(OEt)2CF3 CN NHEt NP(O)Me2CF3 CN NHEt NP(O)Et2CF3 CN NHEt NP(O)Me(OMe)CF3 CN NHEt NP(O)(OPr)2CF3 CN NHEt NC(O)C(O)HCF3 CN NHEt NC(O)C(O)MeCF3 CN NHEt NC(O)C(O)OMeCF3 CN NHEt NC(O)C(O)OEtCF3 CN NHEt NC(O)C(O)NH2CF3 CN NHEt NC(O)C(O)OHCF3 CN NHEt NC(NH)NH2CF3 CN NHEt NC(NOH)NH2CF3 CN NHEt NC(NH)NHMeCF3 CN NHEt NC(NH)NMe2CF3 CN NHEt NC(NH)OMeCF3 CN NHEt NC(NH)OEtCF3 CN NHCOMe NCOMeCF3 CN NHCOMe NCOEtCF3 CN NHCOMe NCOPrCF3 CN NHCOMe NCHOCF3 CN NHCOMe NCOiPrCF3 CN NHCOMe NCOtBuCF3 CN NHCOMe NCOPhCF3 CN NHCOMe NSO2MeCF3 CN NHCOMe NSO2EtCF3 CN NHCOMe NSO2PrCF3 CN NHCOMe NSO2PhCF3 CN NHCOMe NSO2iPrCF3 CN NHCOMe NNO2CF3 CN NHCOMe NCOOMe ¨CF3 CN NHCOMe NCOOEt ¨CF3 CN NHCOMe NCOOPr ¨CF3 CN NHCOMe NCOOiPr ¨CF3 CN NHCOMe NCONHEt ¨CF3 CN NHCOMe NCONHPr ¨CF3 CN NHCOMe NCONH2CF3 CN NHCOMe NCONHMeCF3 CN NHCOMe NCNCF3 CN NHCOMe NCOSMeCF3 CN NHCOMe NCOSEtCF3 CN NHCOMe NCSOMeCF3 CN NHCOMe NCSOEtCF3 CN NHCOMe NCSOPrCF3 CN NHCOMe NSO2NH2CF3 CN NHCOMe NSO2NHMeCF3 CN NHCOMe NSO2NMe2CF3 CN NHCOMe NP(O)(OMe)2CF3 CN NHCOMe NP(O)(OEt)2CF3 CN NHCOMe NP(O)Me2CF3 CN NHCOMe NP(O)Et2CF3 CN NHCOMe NP(O)Me(OMe)CF3 CN NHCOMe NP(O)(OPr)2CF3 CN NHCOMe NC(O)C(O)HCF3 CN NHCOMe NC(O)C(O)MeCF3 CN NHCOMe NC(O)C(O)OMeCF3 CN NHCOMe NC(O)C(O)OEtCF3 CN NHCOMe NC(O)C(O)NH2CF3 CN NHCOMe NC(O)C(O)OHCF3 CN NHCOMe NC(NH)NH2CF3 CN NHCOMe NC(NOH)NH2CF3 CN NHCOMe NC(NH)NHMeCF3 CN NHCOMe NC(NH)NMe2CF3 CN NHCOMe NC(NH)OMeCF3 CN NHCOMe NC(NH)OEtCF3 CN NH2 NCOMe OCF3 CN NH2 NH OCF3 CN NH2 NCOEt OCF3 CN NH2 NCOPr OCF3 CN NH2 NCHO OCF3 CN NH2 NCOiPr OCF3 CN NH2 NCOtBu OCF3 CN NH2 NCOPh OCF3 CN NH2 NSO2Me OCF3 CN NH2 NSO2Et OCF3 CN NH2 NSO2Pr OCF3 CN NH2 NSO2Ph OCF3 CN NH2 NSO2iPr OCF3 CN NH2 NNO2 OCF3 CN NH2 NCOOMe OCF3 CN NH2 NCOOEt OCF3 CN NH2 NCOOPr OCF3 CN NH2 NCOOiPr OCF3 CN NH2 NCONHEt OCF3 CN NH2 NCONHPr OCF3 CN NH2 NCONH2 OCF3 CN NH2 NCONHMe OCF3 CN NH2 NCN OCF3 CN NH2 NCOSMe OCF3 CN NH2 NCOSEt OCF3 CN NH2 NCSOMe OCF3 CN NH2 NCSOEt OCF3 CN NH2 NCSOPr OCF3 CN NH2 NSO2NH2 OCF3 CN NH2 NSO2NHMe OCF3 CN NH2 NSO2NMe2 OCF3 CN NH2 NP(O)(OMe)2 OCF3 CN NH2 NP(O)(OEt)2 OCF3 CN NH2 NP(O)Me2 OCF3 CN NH2 NP(O)Et2 OCF3 CN NH2 NP(O)Me(OMe) OCF3 CN NH2 NP(O)(OPr)2 OCF3 CN NH2 NC(O)C(O)H OCF3 CN NH2 NC(O)C(O)Me OCF3 CN NH2 NC(O)C(O)OMe OCF3 CN NH2 NC(O)C(O)OEt OCF3 CN NH2 NC(O)C(O)NH2 OCF3 CN NH2 NC(O)C(O)OH OCF3 CN NH2 NC(NH)NH2 OCF3 CN NH2 NC(NOH)NH2 OCF3 CN NH2 NC(NH)NHMe OCF3 CN NH2 NC(NH)NMe2 OCF3 CN NH2 NC(NH)OMe OCF3 CN NH2 NC(NH)OEt OCF3 CN NHMe NCOMe OCF3 CN NHMe NCOEt OCF3 CN NHMe NCOPr OCF3 CN NHMe NCHO OCF3 CN NHMe NCOiPr OCF3 CN NHMe NCOtBu OCF3 CN NHMe NCOPh OCF3 CN NHMe NSO2Me OCF3 CN NHMe NSO2Et OCF3 CN NHMe NSO2Pr OCF3 CN NHMe NSO2Ph OCF3 CN NHMe NSO2iPr OCF3 CN NHMe NNO2 OCF3 CN NHMe NCOOMe OCF3 CN NHMe NCOOEt OCF3 CN NHMe NCOOPr OCF3 CN NHMe NCOOiPr OCF3 CN NHMe NCONHEt OCF3 CN NHMe NCONHPr OCF3 CN NHMe NCONH2 OCF3 CN NHMe NCONHMe OCF3 CN NHMe NCN OCF3 CN NHMe NCOSMe OCF3 CN NHMe NCOSEt OCF3 CN NHMe NCSOMe OCF3 CN NHMe NCSOEt OCF3 CN NHMe NCSOPr OCF3 CN NHMe NSO2NH2 OCF3 CN NHMe NSO2NHMe OCF3 CN NHMe NSO2NMe2 OCF3 CN NHMe NP(O)(OMe)2 OCF3 CN NHMe NP(O)(OEt)2 OCF3 CN NHMe NP(O)Me2 OCF3 CN NHMe NP(O)Et2 OCF3 CN NHMe NP(O)Me(OMe) OCF3 CN NHMe NP(O)(OPr)2 OCF3 CN NHMe NC(O)C(O)H OCF3 CN NHMe NC(O)C(O)Me OCF3 CN NHMe NC(O)C(O)OMe OCF3 CN NHMe NC(O)C(O)OEt OCF3 CN NHMe NC(O)C(O)NH2 OCF3 CN NHMe NC(O)C(O)OH OCF3 CN NHMe NC(NH)NH2 OCF3 CN NHMe NC(NOH)NH2 OCF3 CN NHMe NC(NH)NHMe OCF3 CN NHMe NC(NH)NMe2 OCF3 CN NHMe NC(NH)OMe OCF3 CN NHMe NC(NH)OEt OCF3 CN NHEt NCOMe OCF3 CN NHEt NCOEt OCF3 CN NHEt NCOPr OCF3 CN NHEt NCHO OCF3 CN NHEt NCOiPr OCF3 CN NHEt NCOtBu OCF3 CN NHEt NCOPh OCF3 CN NHEt NSO2Me OCF3 CN NHEt NSO2Et OCF3 CN NHEt NSO2Pr OCF3 CN NHEt NSO2Ph OCF3 CN NHEt NSO2iPr OCF3 CN NHEt NNO2 OCF3 CN NHEt NCOOMe OCF3 CN NHEt NCOOEt OCF3 CN NHEt NCOOPr OCF3 CN NHEt NCOOiPr OCF3 CN NHEt NCONHEt OCF3 CN NHEt NCONHPr OCF3 CN NHEt NCONH2 OCF3 CN NHEt NCONHMe OCF3 CN NHEt NCN OCF3 CN NHEt NCOSMe OCF3 CN NHEt NCOSEt OCF3 CN NHEt NCSOMe OCF3 CN NHEt NCSOEt OCF3 CN NHEt NCSOPr OCF3 CN NHEt NSO2NH2 OCF3 CN NHEt NSO2NHMe OCF3 CN NHEt NSO2NMe2 OCF3 CN NHEt NP(O)(OMe)2 OCF3 CN NHEt NP(O)(OEt)2 OCF3 CN NHEt NP(O)Me2 OCF3 CN NHEt NP(O)Et2 OCF3 CN NHEt NP(O)Me(OMe) OCF3 CN NHEt NP(O)(OPr)2 OCF3 CN NHEt NC(O)C(O)H OCF3 CN NHEt NC(O)C(O)Me OCF3 CN NHEt NC(O)C(O)OMe OCF3 CN NHEt NC(O)C(O)OEt OCF3 CN NHEt NC(O)C(O)NH2 OCF3 CN NHEt NC(O)C(O)OH OCF3 CN NHEt NC(NH)NH2 OCF3 CN NHEt NC(NOH)NH2 OCF3 CN NHEt NC(NH)NHMe OCF3 CN NHEt NC(NH)NMe2 OCF3 CN NHEt NC(NH)OMe OCF3 CN NHEt NC(NH)OEt OCCl2F CN NH2 NCOMeCCl2F CN NH2 NCOEtCCl2F CN NH2 NCOPrCCl2F CN NH2 NCHOCCl2F CN NH2 NCOiPrCCl2F CN NH2 NCOtBuCCl2F CN NH2 NCOPhCCl2F CN NH2 NSO2MeCCl2F CN NH2 NSO2EtCCl2F CN NH2 NSO2PrCCl2F CN NH2 NSO2PhCCl2F CN NH2 NSO2iPrCCl2F CN NH2 NNO2CCl2F CN NH2 NCOOMeCCl2F CN NH2 NCOOEtCCl2F CN NH2 NCOOPrCCl2F CN NH2 NCOOiPrCCl2F CN NH2 NCONHEtCCl2F CN NH2 NCONHPrCCl2F CN NH2 NCONH2CCl2F CN NH2 NCONHMeCCl2F CN NH2 NCNCCl2F CN NH2 NCOSMeCCl2F CN NH2 NCOSEtCCl2F CN NH2 NCSOMeCCl2F CN NH2 NCSOEtCCl2F CN NH2 NCSOPrCCl2F CN NH2 NSO2NH2CCl2F CN NH2 NSO2NHMeCCl2F CN NH2 NSO2NMe2CCl2F CN NH2 NP(O)(OMe)2CCl2F CN NH2 NP(O)(OEt)2CCl2F CN NH2 NP(O)Me2CCl2F CN NH2 NP(O)Et2CCl2F CN NH2 NP(O)Me(OMe)CCl2F CN NH2 NP(O)(OPr)2CCl2F CN NH2 NC(O)C(O)HCCl2F CN NH2 NC(O)C(O)MeCCl2F CN NH2 NC(O)C(O)OMeCCl2F CN NH2 NC(O)C(O)OEtCCl2F CN NH2 NC(O)C(O)NH2CCl2F CN NH2 NC(O)C(O)OHCCl2F CN NH2 NC(NH)NH2 ¨CCl2F CN NH2 NC(NOH)NH2 ¨CCl2F CN NH2 NC(NH)NHMe ¨CCl2F CN NH2 NC(NH)NMe2 ¨CCl2F CN NH2 NC(NH)OMe ¨CCl2F CN NH2 NC(NH)OEt ¨CCl2F CN NHMe NCOMe ¨CCl2F CN NHMe NCOEt ¨CCl2F CN NHMe NCOPr ¨CCl2F CN NHMe NCHO ¨CCl2F CN NHMe NCOiPr ¨CCl2F CN NHMe NCOtBuCCl2F CN NHMe NCOPhCCl2F CN NHMe NSO2MeCCl2F CN NHMe NSO2EtCCl2F CN NHMe NSO2PrCCl2F CN NHMe NSO2PhCCl2F CN NHMe NSO2iPrCCl2F CN NHMe NNO2CCl2F CN NHMe NCOOMeCCl2F CN NHMe NCOOEtCCl2F CN NHMe NCOOPrCCl2F CN NHMe NCOOiPrCCl2F CN NHMe NCONHEtCCl2F CN NHMe NCONHPrCCl2F CN NHMe NCONH2CCl2F CN NHMe NCONHMe ¨CCl2F CN NHMe NCN ¨CCl2F CN NHMe NCOSMe ¨CCl2F CN NHMe NCOSEt ¨CCl2F CN NHMe NCSOMe ¨CCl2F CN NHMe NCSOEt ¨CCl2F CN NHMe NCSOPr ¨CCl2F CN NHMe NSO2NH2 ¨CCl2F CN NHMe NSO2NHMe ¨CCl2F CN NHMe NSO2NMe2 ¨CCl2F CN NHMe NP(O)(OMe)2 ¨CCl2F CN NHMe NP(O)(OEt)2 ¨CCl2F CN NHMe NP(O)Me2CCl2F CN NHMe NP(O)Et2CCl2F CN NHMe NP(O)Me(OMe)CCl2F CN NHMe NP(O)(OPr)2CCl2F CN NHMe NC(O)C(O)HCCl2F CN NHMe NC(O)C(O)MeCCl2F CN NHMe NC(O)C(O)OMeCCl2F CN NHMe NC(O)C(O)OEtCCl2F CN NHMe NC(O)C(O)NH2CCl2F CN NHMe NC(O)C(O)OH ¨CCl2F CN NHMe NC(NH)NH2 ¨CCl2F CN NHMe NC(NOH)NH2 ¨CCl2F CN NHMe NC(NH)NHMe ¨CCl2F CN NHMe NC(NH)NMe2 ¨CCl2F CN NHMe NC(NH)OMe ¨CCl2F CN NHMe NC(NH)OEtCCl2F CN NHEt NCOMe ¨CCl2F CN NHEt NCOEtCCl2F CN NHEt NCOPr ¨CCl2F CN NHEt NCHO ¨CCl2F CN NHEt NCOiPr ¨CCl2F CN NHEt NCOtBu ¨CCl2F CN NHEt NCOPh ¨CCl2F CN NHEt NSO2Me ¨CCl2F CN NHEt NSO2Et ¨CCl2F CN NHEt NSO2Pr ¨CCl2F CN NHEt NSO2Ph ¨CCl2F CN NHEt NSO2iPr ¨CCl2F CN NHEt NNO2CCl2F CN NHEt NCOOMeCCl2F CN NHEt NCOOEtCCl2F CN NHEt NCOOPrCCl2F CN NHEt NCOOiPrCCl2F CN NHEt NCONHEtCCl2F CN NHEt NCONHPrCCl2F CN NHEt NCONH2CCl2F CN NHEt NCONHMeCCl2F CN NHEt NCNCCl2F CN NHEt NCOSMeCCl2F CN NHEt NCOSEtCCl2F CN NHEt NCSOMeCCl2F CN NHEt NCSOEtCCl2F CN NHEt NCSOPrCCl2F CN NHEt NSO2NH2CCl2F CN NHEt NSO2NHMe ¨CCl2F CN NHEt NSO2NMe2 ¨CCl2F CN NHEt NP(O)(OMe)2 ¨CCl2F CN NHEt NP(O)(OEt)2 ¨CCl2F CN NHEt NP(O)Me2 ¨CCl2F CN NHEt NP(O)Et2 ¨CCl2F CN NHEt NP(O)Me(OMe ¨CCl2F CN NHEt NP(O)(OPr)2 ¨CCl2F CN NHEt NC(O)C(O)H ¨CCl2F CN NHEt NC(O)C(O)Me ¨CCl2F CN NHEt NC(O)C(O)OMe ¨CCl2F CN NHEt NC(O)C(O)OEtCCl2F CN NHEt NC(O)C(O)NH2CCl2F CN NHEt NC(O)C(O)OHCCl2F CN NHEt NC(NH)NH2CCl2F CN NHEt NC(NOH)NH2CCl2F CN NHEt NC(NH)NHMeCCl2F CN NHEt NC(NH)NMe2CCl2F CN NHEt NC(NH)OMeCCl2F CN NHEt NC(NH)OEtCCl2F CN NH2 NH OCCl2F CN NH2 NCOMe OCCl2F CN NH2 NCOEt OCCl2F CN NH2 NCOPr OCCl2F CN NH2 NCHO OCCl2F CN NH2 NCOiPr OCCl2F CN NH2 NCOtBu OCCl2F CN NH2 NCOPh OCCl2F CN NH2 NSO2Me OCCl2F CN NH2 NSO2Et OCCl2F CN NH2 NSO2Pr OCCl2F CN NH2 NSO2Ph OCCl2F CN NH2 NSO2iPr OCCl2F CN NH2 NNO2 OCCl2F CN NH2 NCOOMe OCCl2F CN NH2 NCOOEt OCCl2F CN NH2 NCOOPr OCCl2F CN NH2 NCOOiPr OCCl2F CN NH2 NCONHEt OCCl2F CN NH2 NCONHPr OCCl2F CN NH2 NCONH2 OCCl2F CN NH2 NCONHMe OCCl2F CN NH2 NCN OCCl2F CN NH2 NCOSMe OCCl2F CN NH2 NCOSEt OCCl2F CN NH2 NCSOMe OCCl2F CN NH2 NCSOEt OCCl2F CN NH2 NCSOPr OCCl2F CN NH2 NSO2NH2 OCCl2F CN NH2 NSO2NHMe OCCl2F CN NH2 NSO2NMe2 OCCl2F CN NH2 NP(O)(OMe)2 OCCl2F CN NH2 NP(O)(OEt)2 OCCl2F CN NH2 NP(O)Me2 OCCl2F CN NH2 NP(O)Et2 OCCl2F CN NH2 NP(O)Me(OMe) OCCl2F CN NH2 NP(O)(OPr)2 OCCl2F CN NH2 NC(O)C(O)H OCCl2F CN NH2 NC(O)C(O)Me OCCl2F CN NH2 NC(O)C(O)OMe OCCl2F CN NH2 NC(O)C(O)OEt OCCl2F CN NH2 NC(O)C(O)NH2 OCCl2F CN NH2 NC(O)C(O)OH OCCl2F CN NH2 NC(NH)NH2 OCCl2F CN NH2 NC(NOH)NH2 OCCl2F CN NH2 NC(NH)NHMe OCCl2F CN NH2 NC(NH)NMe2 OCCl2F CN NH2 NC(NH)OMe OCCl2F CN NH2 NC(NH)OEt OCCl2F CN NHMe NCOMe OCCl2F CN NHMe NCOEt OCCl2F CN NHMe NCOPr OCCl2F CN NHMe NCHO OCCl2F CN NHMe NCOiPr OCCl2F CN NHMe NCOtBu OCCl2F CN NHMe NCOPh OCCl2F CN NHMe NSO2Me OCCl2F CN NHMe NSO2Et OCCl2F CN NHMe NSO2Pr OCCl2F CN NHMe NSO2Ph OCCl2F CN NHMe NSO2iPr OCCl2F CN NHMe NNO2 OCCl2F CN NHMe NCOOMe OCCl2F CN NHMe NCOOEt OCCl2F CN NHMe NCOOPr OCCl2F CN NHMe NCOOiPr OCCl2F CN NHMe NCONHEt OCCl2F CN NHMe NCONHPr OCCl2F CN NHMe NCONH2 OCCl2F CN NHMe NCONHMe OCCl2F CN NHMe NCN OCCl2F CN NHMe NCOSMe OCCl2F CN NHMe NCOSEt OCCl2F CN NHMe NCSOMe OCCl2F CN NHMe NCSOEt OCCl2F CN NHMe NCSOPr OCCl2F CN NHMe NSO2NH2 OCCl2F CN NHMe NSO2NHMe OCCl2F CN NHMe NSO2NMe2 OCCl2F CN NHMe NP(O)(OMe)2 OCCl2F CN NHMe NP(O)(OEt)2 OCCl2F CN NHMe NP(O)Me2 OCCl2F CN NHMe NP(O)Et2 OCCl2F CN NHMe NP(O)Me(OMe) OCCl2F CN NHMe NP(O)(OPr)2 OCCl2F CN NHMe NC(O)C(O)H OCCl2F CN NHMe NC(O)C(O)Me OCCl2F CN NHMe NC(O)C(O)OMe OCCl2F CN NHMe NC(O)C(O)OEt OCCl2F CN NHMe NC(O)C(O)NH2 OCCl2F CN NHMe NC(O)C(O)OH OCCl2F CN NHMe NC(NH)NH2 OCCl2F CN NHMe NC(NOH)NH2 OCCl2F CN NHMe NC(NH)NHMe OCCl2F CN NHMe NC(NH)NMe2 OCCl2F CN NHMe NC(NH)OMe OCCl2F CN NHMe NC(NH)OEt OCCl2F CN NHEt NCOMe OCCl2F CN NHEt NCOEt OCCl2F CN NHEt NCOPr OCCl2F CN NHEt NCHO OCCl2F CN NHEt NCOiPr OCCl2F CN NHEt NCOtBu OCCl2F CN NHEt NCOPh OCCl2F CN NHEt NSO2Me OCCl2F CN NHEt NSO2Et OCCl2F CN NHEt NSO2Pr OCCl2F CN NHEt NSO2Ph OCCl2F CN NHEt NSO2iPr OCCl2F CN NHEt NNO2 OCCl2F CN NHEt NCOOMe OCCl2F CN NHEt NCOOEt OCCl2F CN NHEt NCOOPr OCCl2F CN NHEt NCOOiPr OCCl2F CN NHEt NCONHEt OCCl2F CN NHEt NCONHPr OCCl2F CN NHEt NCONH2 OCCl2F CN NHEt NCONHMe OCCl2F CN NHEt NCN OCCl2F CN NHEt NCOSMe OCCl2F CN NHEt NCOSEt OCCl2F CN NHEt NCSOMe OCCl2F CN NHEt NCSOEt OCCl2F CN NHEt NCSOPr OCCl2F CN NHEt NSO2NH2 OCCl2F CN NHEt NSO2NHMe OCCl2F CN NHEt NSO2NMe2 OCCl2F CN NHEt NP(O)(OMe)2 OCCl2F CN NHEt NP(O)(OEt)2 OCCl2F CN NHEt NP(O)Me2 OCCl2F CN NHEt NP(O)Et2 OCCl2F CN NHEt NP(O)Me(OMe) OCCl2F CN NHEt NP(O)(OPr)2 OCCl2F CN NHEt NC(O)C(O)H OCCl2F CN NHEt NC(O)C(O)Me OCCl2F CN NHEt NC(O)C(O)OMe OCCl2F CN NHEt NC(O)C(O)OEt OCCl2F CN NHEt NC(O)C(O)NH2 OCCl2F CN NHEt NC(O)C(O)OH OCCl2F CN NHEt NC(NH)NH2 OCCl2F CN NHEt NC(NOH)NH2 OCCl2F CN NHEt NC(NH)NHMe OCCl2F CN NHEt NC(NH)NMe2 OCCl2F CN NHEt NC(NH)OMe OCCl2F CN NHEt NC(NH)OEt OCF2Cl CN NH2 NCOMeCF2Cl CN NH2 NCOEtCF2Cl CN NH2 NCOPrCF2Cl CN NH2 NCHO ¨CF2Cl CN NH2 NCOiPr ¨CF2Cl CN NH2 NCOtBu ¨CF2Cl CN NH2 NCOPh ¨CF2Cl CN NH2 NSO2Me ¨CF2Cl CN NH2 NSO2Et ¨CF2Cl CN NH2 NSO2Pr ¨CF2Cl CN NH2 NSO2Ph ¨CF2Cl CN NH2 NSO2iPr ¨CF2Cl CN NH2 NNO2 ¨CF2Cl CN NH2 NCOOMe ¨CF2Cl CN NH2 NCOOEt ¨CF2Cl CN NH2 NCOOPr ¨CF2Cl CN NH2 NCOOiPr ¨CF2Cl CN NH2 NCONHEt ¨CF2Cl CN NH2 NCONHPrCF2Cl CN NH2 NCONH2CF2Cl CN NH2 NCONHMeCF2Cl CN NH2 NCN ¨CF2Cl CN NH2 NCOSMe ¨CF2Cl CN NH2 NCOSEtCF2Cl CN NH2 NCSOMe ¨CF2Cl CN NH2 NCSOEt ¨CF2Cl CN NH2 NCSOPrCF2Cl CN NH2 NSO2NH2 ¨CF2Cl CN NH2 NSO2NHMe ¨CF2Cl CN NH2 NSO2NMe2CF2Cl CN NH2 NP(O)(OMe)2CF2Cl CN NH2 NP(O)(OEt)2 ¨CF2Cl CN NH2 NP(O)Me2 ¨CF2Cl CN NH2 NP(O)Et2 ¨CF2Cl CN NH2 NP(O)Me(OMe) ¨CF2Cl CN NH2 NP(O)(OPr)2 ¨CF2Cl CN NH2 NC(O)C(O)H ¨CF2Cl CN NH2 NC(O)C(O)Me ¨CF2Cl CN NH2 NC(O)C(O)OMe ¨CF2Cl CN NH2 NC(O)C(O)OEt ¨CF2Cl CN NH2 NC(O)C(O)NH2 ¨CF2Cl CN NH2 NC(O)C(O)OH ¨CF2Cl CN NH2 NC(NH)NH2 ¨CF2Cl CN NH2 NC(NOH)NH2CF2Cl CN NH2 NC(NH)NHMeCF2Cl CN NH2 NC(NH)NMe2CF2Cl CN NH2 NC(NH)OMeCF2Cl CN NH2 NC(NH)OEtCF2Cl CN NHMe NCOMeCF2Cl CN NHMe NCOEtCF2Cl CN NHMe NCOPrCF2Cl CN NHMe NCHOCF2Cl CN NHMe NCOiPrCF2Cl CN NHMe NCOtBuCF2Cl CN NHMe NCOPhCF2Cl CN NHMe NSO2MeCF2Cl CN NHMe NSO2EtCF2Cl CN NHMe NSO2PrCF2Cl CN NHMe NSO2PhCF2Cl CN NHMe NSO2iPr ¨CF2Cl CN NHMe NNO2 ¨CF2Cl CN NHMe NCOOMe ¨CF2Cl CN NHMe NCOOEt ¨CF2Cl CN NHMe NCOOPr ¨CF2Cl CN NHMe NCOOiPr ¨CF2Cl CN NHMe NCONHEt ¨CF2Cl CN NHMe NCONHPr ¨CF2Cl CN NHMe NCONH2 ¨CF2Cl CN NHMe NCONHMe ¨CF2Cl CN NHMe NCN ¨CF2Cl CN NHMe NCOSMe ¨CF2Cl CN NHMe NCOSEt ¨CF2Cl CN NHMe NCSOMeCF2Cl CN NHMe NCSOEtCF2Cl CN NHMe NCSOPrCF2Cl CN NHMe NSO2NH2CF2Cl CN NHMe NSO2NHMeCF2Cl CN NHMe NSO2NMe2CF2Cl CN NHMe NP(O)(OMe)2CF2Cl CN NHMe NP(O)(OEt)2CF2Cl CN NHMe NP(O)Me2CF2Cl CN NHMe NP(O)Et2CF2Cl CN NHMe NP(O)Me(OMe)CF2Cl CN NHMe NP(O)(OPr)2CF2Cl CN NHMe NC(O)C(O)HCF2Cl CN NHMe NC(O)C(O)MeCF2Cl CN NHMe NC(O)C(O)OMeCF2Cl CN NHMe NC(O)C(O)OEtCF2Cl CN NHMe NC(O)C(O)NH2CF2Cl CN NHMe NC(O)C(O)OH ¨CF2Cl CN NHMe NC(NH)NH2 ¨CF2Cl CN NHMe NC(NOH)NH2 ¨CF2Cl CN NHMe NC(NH)NHMe ¨CF2Cl CN NHMe NC(NH)NMe2 ¨CF2Cl CN NHMe NC(NH)OMe ¨CF2Cl CN NHMe NC(NH)OEt ¨CF2Cl CN NHEt NCOMe ¨CF2Cl CN NHEt NCOEt ¨CF2Cl CN NHEt NCOPr ¨CF2Cl CN NHEt NCHOCF2Cl CN NHEt NCOiPrCF2Cl CN NHEt NCOtBuCF2Cl CN NHEt NCOPhCF2Cl CN NHEt NSO2MeCF2Cl CN NHEt NSO2EtCF2Cl CN NHEt NSO2PrCF2Cl CN NHEt NSO2PhCF2Cl CN NHEt NSO2iPrCF2Cl CN NHEt NNO2CF2Cl CN NHEt NCOOMeCF2Cl CN NHEt NCOOEtCF2Cl CN NHEt NCOOPrCF2Cl CN NHEt NCOOiPrCF2Cl CN NHEt NCONHEtCF2Cl CN NHEt NCONHPrCF2Cl CN NHEt NCONH2CF2Cl CN NHEt NCONHMeCF2Cl CN NHEt NCN ¨CF2Cl CN NHEt NCOSMe ¨CF2Cl CN NHEt NCOSEtCF2Cl CN NHEt NCSOMe ¨CF2Cl CN NHEt NCSOEt ¨CF2Cl CN NHEt NCSOPr ¨CF2Cl CN NHEt NSO2NH2 ¨CF2Cl CN NHEt NSO2NHMe ¨CF2Cl CN NHEt NSO2NMe2CF2Cl CN NHEt NP(O)(OMe)2CF2Cl CN NHEt NP(O)(OEt)2CF2Cl CN NHEt NP(O)Me2CF2Cl CN NHEt NP(O)Et2CF2Cl CN NHEt NP(O)Me(OMe)CF2Cl CN NHEt NP(O)(OPr)2CF2Cl CN NHEt NC(O)C(O)HCF2Cl CN NHEt NC(O)C(O)MeCF2Cl CN NHEt NC(O)C(O)OMeCF2Cl CN NHEt NC(O)C(O)OEtCF2Cl CN NHEt NC(O)C(O)NH2CF2Cl CN NHEt NC(O)C(O)OHCF2Cl CN NHEt NC(NH)NH2CF2Cl CN NHEt NC(NOH)NH2CF2Cl CN NHEt NC(NH)NHMeCF2Cl CN NHEt NC(NH)NMe2CF2Cl CN NHEt NC(NH)OMeCF2Cl CN NHEt NC(NH)OEtCF2Cl CN NH2 NH OCF2Cl CN NH2 NCOMe OCF2Cl CN NH2 NCOEt OCF2Cl CN NH2 NCOPr OCF2Cl CN NH2 NCHO OCF2Cl CN NH2 NCOiPr OCF2Cl CN NH2 NCOtBu OCF2Cl CN NH2 NCOPh OCF2Cl CN NH2 NSO2Me OCF2Cl CN NH2 NSO2Et OCF2Cl CN NH2 NSO2Pr OCF2Cl CN NH2 NSO2Ph OCF2Cl CN NH2 NSO2iPr OCF2Cl CN NH2 NNO2 OCF2Cl CN NH2 NCOOMe OCF2Cl CN NH2 NCOOEt OCF2Cl CN NH2 NCOOPr OCF2Cl CN NH2 NCOOiPr OCF2Cl CN NH2 NCONHEt OCF2Cl CN NH2 NCONHPr OCF2Cl CN NH2 NCONH2 OCF2Cl CN NH2 NCONHMe OCF2Cl CN NH2 NCN OCF2Cl CN NH2 NCOSMe OCF2Cl CN NH2 NCOSEt OCF2Cl CN NH2 NCSOMe OCF2Cl CN NH2 NCSOEt OCF2Cl CN NH2 NCSOPr OCF2Cl CN NH2 NSO2NH2 OCF2Cl CN NH2 NSO2NHMe OCF2Cl CN NH2 NSO2NMe2 OCF2Cl CN NH2 NP(O)(OMe)2 OCF2Cl CN NH2 NP(O)(OEt)2 OCF2Cl CN NH2 NP(O)Me2 OCF2Cl CN NH2 NP(O)Et2 OCF2Cl CN NH2 NP(O)Me(OMe) OCF2Cl CN NH2 NP(O)(OPr)2 OCF2Cl CN NH2 NC(O)C(O)H OCF2Cl CN NH2 NC(O)C(O)Me OCF2Cl CN NH2 NC(O)C(O)OMe OCF2Cl CN NH2 NC(O)C(O)OEt OCF2Cl CN NH2 NC(O)C(O)NH2 OCF2Cl CN NH2 NC(O)C(O)OH OCF2Cl CN NH2 NC(NH)NH2 OCF2Cl CN NH2 NC(NOH)NH2 OCF2Cl CN NH2 NC(NH)NHMe OCF2Cl CN NH2 NC(NH)NMe2 OCF2Cl CN NH2 NC(NH)OMe OCF2Cl CN NH2 NC(NH)OEt OCF2Cl CN NHMe NCOMe OCF2Cl CN NHMe NCOEt OCF2Cl CN NHMe NCOPr OCF2Cl CN NHMe NCHO OCF2Cl CN NHMe NCOiPr OCF2Cl CN NHMe NCOtBu OCF2Cl CN NHMe NCOPh OCF2Cl CN NHMe NSO2Me OCF2Cl CN NHMe NSO2Et OCF2Cl CN NHMe NSO2Pr OCF2Cl CN NHMe NSO2Ph OCF2Cl CN NHMe NSO2iPr OCF2Cl CN NHMe NNO2 OCF2Cl CN NHMe NCOOMe OCF2Cl CN NHMe NCOOEt OCF2Cl CN NHMe NCOOPr OCF2Cl CN NHMe NCOOiPr OCF2Cl CN NHMe NCONHEt OCF2Cl CN NHMe NCONHPr OCF2Cl CN NHMe NCONH2 OCF2Cl CN NHMe NCONHMe OCF2Cl CN NHMe NCN OCF2Cl CN NHMe NCOSMe OCF2Cl CN NHMe NCOSEt OCF2Cl CN NHMe NCSOMe OCF2Cl CN NHMe NCSOEt OCF2Cl CN NHMe NCSOPr OCF2Cl CN NHMe NSO2NH2 OCF2Cl CN NHMe NSO2NHMe OCF2Cl CN NHMe NSO2NMe2 OCF2Cl CN NHMe NP(O)(OMe)2 OCF2Cl CN NHMe NP(O)(OEt)2 OCF2Cl CN NHMe NP(O)Me2 OCF2Cl CN NHMe NP(O)Et2 OCF2Cl CN NHMe NP(O)Me(OMe) OCF2Cl CN NHMe NP(O)(OPr)2 OCF2Cl CN NHMe NC(O)C(O)H OCF2Cl CN NHMe NC(O)C(O)Me OCF2Cl CN NHMe NC(O)C(O)OMe OCF2Cl CN NHMe NC(O)C(O)OEt OCF2Cl CN NHMe NC(O)C(O)NH2 OCF2Cl CN NHMe NC(O)C(O)OH OCF2Cl CN NHMe NC(NH)NH2 OCF2Cl CN NHMe NC(NOH)NH2 OCF2Cl CN NHMe NC(NH)NHMe OCF2Cl CN NHMe NC(NH)NMe2 OCF2Cl CN NHMe NC(NH)OMe OCF2Cl CN NHMe NC(NH)OEt OCF2Cl CN NHEt NCOMe OCF2Cl CN NHEt NCOEt OCF2Cl CN NHEt NCOPr OCF2Cl CN NHEt NCHO OCF2Cl CN NHEt NCOiPr OCF2Cl CN NHEt NCOtBu OCF2Cl CN NHEt NCOPh OCF2Cl CN NHEt NSO2Me OCF2Cl CN NHEt NSO2Et OCF2Cl CN NHEt NSO2Pr OCF2Cl CN NHEt NSO2Ph OCF2Cl CN NHEt NSO2iPr OCF2Cl CN NHEt NNO2 OCF2Cl CN NHEt NCOOMe OCF2Cl CN NHEt NCOOEt OCF2Cl CN NHEt NCOOPr OCF2Cl CN NHEt NCOOiPr OCF2Cl CN NHEt NCONHEt OCF2Cl CN NHEt NCONHPr OCF2Cl CN NHEt NCONH2 OCF2Cl CN NHEt NCONHMe OCF2Cl CN NHEt NCN OCF2Cl CN NHEt NCOSMe OCF2Cl CN NHEt NCOSEt OCF2Cl CN NHEt NCSOMe OCF2Cl CN NHEt NCSOEt OCF2Cl CN NHEt NCSOPr OCF2Cl CN NHEt NSO2NH2 OCF2Cl CN NHEt NSO2NHMe OCF2Cl CN NHEt NSO2NMe2 OCF2Cl CN NHEt NP(O)(OMe)2 OCF2Cl CN NHEt NP(O)(OEt)2 OCF2Cl CN NHEt NP(O)Me2 OCF2Cl CN NHEt NP(O)Et2 OCF2Cl CN NHEt NP(O)Me(OMe) OCF2Cl CN NHEt NP(O)(OPr)2 OCF2Cl CN NHEt NC(O)C(O)H OCF2Cl CN NHEt NC(O)C(O)Me OCF2Cl CN NHEt NC(O)C(O)OMe OCF2Cl CN NHEt NC(O)C(O)OEt OCF2Cl CN NHEt NC(O)C(O)NH2 OCF2Cl CN NHEt NC(O)C(O)OH OCF2Cl CN NHEt NC(NH)NH2 OCF2Cl CN NHEt NC(NOH)NH2 OCF2Cl CN NHEt NC(NH)NHMe OCF2Cl CN NHEt NC(NH)NMe2 OCF2Cl CN NHEt NC(NH)OMe OCF2Cl CN NHEt NC(NH)OEt OCF3 CN H NCOMe ¨CF3 CN H NCOEt ¨CF3 CN H NCOPr ¨CF3 CN H NCHO ¨CF3 CN H NCOiPr ¨CF3 CN H NCOtBu ¨CF3 CN H NCOPhCF3 CN H NSO2MeCF3 CN H NSO2Et ¨CF3 CN H NSO2PrCF3 CN H NSO2PhCF3 CN H NSO2iPrCF3 CN H NNO2CF3 CN H NCOOMeCF3 CN H NCOOEtCF3 CN H NCOOPrCF3 CN H NCOOiPrCF3 CN H NCONHEtCF3 CN H NCONHPrCF3 CN H NCONH2CF3 CN H NCONHMeCF3 CN H NCNCF3 CN H NCOSMeCF3 CN H NCOSEt ¨CF3 CN H NCSOMe ¨CF3 CN H NCSOEt ¨CF3 CN H NCSOPr ¨CF3 CN H NSO2NH2 ¨CF3 CN H NSO2NHMe ¨CF3 CN H NSO2NMe2 ¨CF3 CN H NP(O)(OMe)2 ¨CF3 CN H NP(O)(OEt)2 ¨CF3 CN H NP(O)Me2 ¨CF3 CN H NP(O)Et2 ¨CF3 CN H NP(O)Me(OMe)CF3 CN H NP(O)(OPr)2CF3 CN H NC(O)C(O)HCF3 CN H NC(O)C(O)MeCF3 CN H NC(O)C(O)OMeCF3 CN H NC(O)C(O)OEtCF3 CN H NC(O)C(O)NH2CF3 CN H NC(O)C(O)OHCF3 CN H NC(NH)NH2CF3 CN H NC(NOH)NH2CF3 CN H NC(NH)NHMe ¨CF3 CN H NC(NH)NMe2CF3 CN H NC(NH)OMeCF3 CN H NC(NH)OEtCF3 CN H NH OCF3 CN H NCOMe OCF3 CN H NCOEt OCF3 CN H NCOPr OCF3 CN H NCHO OCF3 CN H NCOiPr OCF3 CN H NCOtBu OCF3 CN H NCOPh OCF3 CN H NSO2Me OCF3 CN H NSO2Et OCF3 CN H NSO2Pr OCF3 CN H NSO2Ph OCF3 CN H NSO2iPr OCF3 CN H NNO2 OCF3 CN H NCOOMe OCF3 CN H NCOOEt OCF3 CN H NCOOPr OCF3 CN H NCOOiPr OCF3 CN H NCONHEt OCF3 CN H NCONHPr OCF3 CN H NCONH2 OCF3 CN H NCONHMe OCF3 CN H NCN OCF3 CN H NCOSMe OCF3 CN H NCOSEt OCF3 CN H NCSOMe OCF3 CN H NCSOEt OCF3 CN H NCSOPr OCF3 CN H NSO2NH2 OCF3 CN H NSO2NHMe OCF3 CN H NSO2NMe2 OCF3 CN H NP(O)(OMe)2 OCF3 CN H NP(O)(OEt)2 OCF3 CN H NP(O)Me2 OCF3 CN H NP(O)Et2 OCF3 CN H NP(O)Me(OMe) OCF3 CN H NP(O)(OPr)2 OCF3 CN H NC(O)C(O)H OCF3 CN H NC(O)C(O)Me OCF3 CN H NC(O)C(O)OMe OCF3 CN H NC(O)C(O)OEt OCF3 CN H NC(O)C(O)NH2 OCF3 CN H NC(O)C(O)OH OCF3 CN H NC(NH)NH2 OCF3 CN H NC(NOH)NH2 OCF3 CN H NC(NH)NHMe OCF3 CN H NC(NH)NMe2 OCF3 CN H NC(NH)OMe OCF3 CN H NC(NH)OEt OCF3 CN Me NCOMeCF3 CN Me NCOEtCF3 CN Me NCOPrCF3 CN Me NCHOCF3 CN Me NCOiPr ¨CF3 CN Me NCOtBu ¨CF3 CN Me NCOPh ¨CF3 CN Me NSO2MeCF3 CN Me NSO2EtCF3 CN Me NSO2PrCF3 CN Me NSO2Ph ¨CF3 CN Me NSO2iPr ¨CF3 CN Me NNO2 ¨CF3 CN Me NCOOMe ¨CF3 CN Me NCOOEt ¨CF3 CN Me NCOOPr ¨CF3 CN Me NCOOiPr ¨CF3 CN Me NCONHEt ¨CF3 CN Me NCONHPr ¨CF3 CN Me NCOH ¨CF3 CN Me NCONHMe ¨CF3 CN Me NCN ¨CF3 CN Me NCOSMe ¨CF3 CN Me NCOSEt ¨CF3 CN Me NCSOMe ¨CF3 CN Me NCSOEt ¨CF3 CN Me NCSOPrCF3 CN Me NSO2HCF3 CN Me NSO2NHMeCF3 CN Me NSO2NMe2CF3 CN Me NP(O)(OMe)2CF3 CN Me NP(O)(OEt)2 ¨CF3 CN Me NP(O)Me2 ¨CF3 CN Me NP(O)Et2 ¨CF3 CN Me NP(O)Me(OMe) ¨CF3 CN Me NP(O)(OPr)2CF3 CN Me NC(O)C(O)H ¨CF3 CN Me NC(O)C(O)MeCF3 CN Me NC(O)C(O)OMeCF3 CN Me NC(O)C(O)OEtCF3 CN Me NC(O)C(O)NH2 ¨CF3 CN Me NC(O)C(O)OH ¨CF3 CN Me NC(NH)H ¨CF3 CN Me NC(NOH)H ¨CF3 CN Me NC(NH)NHM ¨CF3 CN Me NC(NH)NMe ¨CF3 CN Me NC(NH)OMe ¨CF3 CN Me NC(NH)OEt ¨CF3 CN Me NH OCF3 CN Me NCOMe OCF3 CN Me NCOEt OCF3 CN Me NCOPr OCF3 CN Me NCHO OCF3 CN Me NCOiPr OCF3 CN Me NCOtBu OCF3 CN Me NCOPh OCF3 CN Me NSO2Me OCF3 CN Me NSO2Et OCF3 CN Me NSO2Pr OCF3 CN Me NSO2Ph OCF3 CN Me NSO2iPr OCF3 CN Me NNO2 OCF3 CN Me NCOOMe OCF3 CN Me NCOOEt OCF3 CN Me NCOOPr OCF3 CN Me NCOOiPr OCF3 CN Me NCONHEt OCF3 CN Me NCONHPr OCF3 CN Me NCONH2 OCF3 CN Me NCONHMe OCF3 CN Me NCN OCF3 CN Me NCOSMe OCF3 CN Me NCOSEt OCF3 CN Me NCSOMe OCF3 CN Me NCSOEt OCF3 CN Me NCSOPr OCF3 CN Me NSO2NH2 OCF3 CN Me NSO2NHMe OCF3 CN Me NSO2NMe2 OCF3 CN Me NP(O)(OMe)2 OCF3 CN Me NP(O)(OEt)2 OCF3 CN Me NP(O)Me2 OCF3 CN Me NP(O)Et2 OCF3 CN Me NP(O)Me(OMe) OCF3 CN Me NP(O)(OPr)2 OCF3 CN Me NC(O)C(O)H OCF3 CN Me NC(O)C(O)Me OCF3 CN Me NC(O)C(O)OMe OCF3 CN Me NC(O)C(O)OEt OCF3 CN Me NC(O)C(O)NH2 OCF3 CN Me NC(O)C(O)OH OCF3 CN Me NC(NH)NH2 OCF3 CN Me NC(NOH)NH2 OCF3 CN Me NC(NH)NHMe OCF3 CN Me NC(NH)NMe2 OCF3 CN Me NC(NH)OMe OCF3 CN Me NC(NH)OEt OCF3 CN Cl NCOMe ¨CF3 CN Cl NCOEt ¨CF3 CN Cl NCOPr ¨CF3 CN Cl NCHO ¨CF3 CN Cl NCOiPr ¨CF3 CN Cl NCOtBu ¨CF3 CN Cl NCOPh ¨CF3 CN Cl NSO2Me ¨CF3 CN Cl NSO2Et ¨CF3 CN Cl NSO2Pr ¨CF3 CN Cl NSO2Ph ¨CF3 CN Cl NSO2iPrCF3 CN Cl NNO2 ¨CF3 CN Cl NCOOMeCF3 CN Cl NCOOEtCF3 CN Cl NCOOPrCF3 CN Cl NCOOiPrCF3 CN Cl NCONHEt ¨CF3 CN Cl NCONHPr ¨CF3 CN Cl NCOHCF3 CN Cl NCONHMeCF3 CN Cl NCN ¨CF3 CN Cl NCOSMe ¨CF3 CN Cl NCOSEt ¨CF3 CN Cl NCSOMeCF3 CN Cl NCSOEtCF3 CN Cl NCSOPr ¨CF3 CN Cl NSO2H ¨CF3 CN Cl NSO2NHMe ¨CF3 CN Cl NSO2NMe2 ¨CF3 CN Cl NP(O)(OMe)2 ¨CF3 CN Cl NP(O)(OEt)2 ¨CF3 CN Cl NP(O)Me2 ¨CF3 CN Cl NP(O)Et2 ¨CF3 CN Cl NP(O)Me(OMe) ¨CF3 CN Cl NP(O)(OPr)2CF3 CN Cl NC(O)C(O)HCF3 CN Cl NC(O)C(O)MeCF3 CN Cl NC(O)C(O)OMeCF3 CN Cl NC(O)C(O)OEtCF3 CN Cl NC(O)C(O)NH2CF3 CN Cl NC(O)C(O)OHCF3 CN Cl NC(NH)HCF3 CN Cl NC(NOH)HCF3 CN Cl NC(NH)NHMeCF3 CN Cl NC(NH)NMe2CF3 CN Cl NC(NH)OMeCF3 CN Cl NC(NH)OEtCF3 CN Cl NCOMe OCF3 CN Cl NCOEt OCF3 CN Cl NCOPr OCF3 CN Cl NCHO OCF3 CN Cl NCOiPr OCF3 CN Cl NCOtBu OCF3 CN Cl NCOPh OCF3 CN Cl NSO2Me OCF3 CN Cl NSO2Et OCF3 CN Cl NSO2Pr OCF3 CN Cl NSO2Ph OCF3 CN Cl NSO2iPr OCF3 CN Cl NNO2 OCF3 CN Cl NCOOMe OCF3 CN Cl NCOOEt OCF3 CN Cl NCOOPr OCF3 CN Cl NCOOiPr OCF3 CN Cl NCONHEt OCF3 CN Cl NCONHPr OCF3 CN Cl NCONH2 OCF3 CN Cl NCONHMe OCF3 CN Cl NCN OCF3 CN Cl NCOSMe OCF3 CN Cl NCOSEt OCF3 CN Cl NCSOMe OCF3 CN Cl NCSOEt OCF3 CN Cl NCSOPr OCF3 CN Cl NSO2NH2 OCF3 CN Cl NSO2NHMe OCF3 CN Cl NSO2NMe2 OCF3 CN Cl NP(O)(OMe)2 OCF3 CN Cl NP(O)(OEt)2 OCF3 CN Cl NP(O)Me2 OCF3 CN Cl NP(O)Et2 OCF3 CN Cl NP(O)Me(OMe) OCF3 CN Cl NP(O)(OPr)2 OCF3 CN Cl NC(O)C(O)H OCF3 CN Cl NC(O)C(O)Me OCF3 CN Cl NC(O)C(O)OMe OCF3 CN Cl NC(O)C(O)OEt OCF3 CN Cl NC(O)C(O)NH2 OCF3 CN Cl NC(O)C(O)OH OCF3 CN Cl NC(NH)NH2 OCF3 CN Cl NC(NOH)NH2 OCF3 CN Cl NC(NH)NHMe OCF3 CN Cl NC(NH)NMe2 OCF3 CN Cl NC(NH)OMe OCF3 CN Cl NC(NH)OEt OCF3 CN SMe NCOMeCF3 CN SMe NCOEtCF3 CN SMe NCOPrCF3 CN SMe NCHOCF3 CN SMe NCOiPrCF3 CN SMe NCOtBuCF3 CN SMe NCOPhCF3 CN SMe NSO2MeCF3 CN SMe NSO2EtCF3 CN SMe NSO2PrCF3 CN SMe NSO2PhCF3 CN SMe NSO2iPrCF3 CN SMe NNO2 ¨CF3 CN SMe NCOOMe ¨CF3 CN SMe NCOOEt ¨CF3 CN SMe NCOOPr ¨CF3 CN SMe NCOOiPr ¨CF3 CN SMe NCONHEt ¨CF3 CN SMe NCONHPr ¨CF3 CN SMe NCOH ¨CF3 CN SMe NCONHMe ¨CF3 CN SMe NCN ¨CF3 CN SMe NCOSMe ¨CF3 CN SMe NCOSEt ¨CF3 CN SMe NCSOMeCF3 CN SMe NCSOEtCF3 CN SMe NCSOPrCF3 CN SMe NSO2HCF3 CN SMe NSO2NHMeCF3 CN SMe NSO2NMe2CF3 CN SMe NP(O)(OMe)2CF3 CN SMe NP(O)(OEt)2CF3 CN SMe NP(O)Me2CF3 CN SMe NP(O)Et2 ¨CF3 CN SMe NP(O)Me(OMe) ¨CF3 CN SMe NP(O)(OPr)2 ¨CF3 CN SMe NC(O)C(O)H ¨CF3 CN SMe NC(O)C(O)Me ¨CF3 CN SMe NC(O)C(O)OMe ¨CF3 CN SMe NC(O)C(O)OEt ¨CF3 CN SMe NC(O)C(O)NH2CF3 CN SMe NC(O)C(O)OHCF3 CN SMe NC(NH)H ¨CF3 CN SMe NC(NOH)H ¨CF3 CN SMe NC(NH)NHMe ¨CF3 CN SMe NC(NH)NMe2 ¨CF3 CN SMe NC(NH)OMe ¨CF3 CN SMe NC(NH)OEt ¨CF3 H NH2 NCOMe ¨CF3 H NH2 NCOEt ¨CF3 H NH2 NCOPr ¨CF3 H NH2 NCHO ¨CF3 H NH2 NCOiPrCF3 H NH2 NCOtBuCF3 H NH2 NCOPhCF3 H NH2 NSO2MeCF3 H NH2 NSO2EtCF3 H NH2 NSO2PrCF3 H NH2 NSO2PhCF3 H NH2 NSO2iPrCF3 H NH2 NNO2CF3 H NH2 NCOOMeCF3 H NH2 NCOOEt ¨CF3 H NH2 NCOOPrCF3 H NH2 NCOOiPr ¨CF3 H NH2 NCONHEt ¨CF3 H NH2 NCONHPrCF3 H NH2 NCOH ¨CF3 H NH2 NCONHMeCF3 H NH2 NCN ¨CF3 H NH2 NCOSMe ¨CF3 H NH2 NCOSEt ¨CF3 H NH2 NCSOMe ¨CF3 H NH2 NCSOEt ¨CF3 H NH2 NCSOPr ¨CF3 H NH2 NSO2H ¨CF3 H NH2 NSO2NHMe ¨CF3 H NH2 NSO2NMe2 ¨CF3 H NH2 NP(O)(OMe)2 ¨CF3 H NH2 NP(O)(OEt)2 ¨CF3 H NH2 NP(O)Me2CF3 H NH2 NP(O)Et2CF3 H NH2 NP(O)Me(OMe)CF3 H NH2 NP(O)(OPr)2CF3 H NH2 NC(O)C(O)HCF3 H NH2 NC(O)C(O)MeCF3 H NH2 NC(O)C(O)OMeCF3 H NH2 NC(O)C(O)OEtCF3 H NH2 NC(O)C(O)NH2CF3 H NH2 NC(O)C(O)OHCF3 H NH2 NC(NH)HCF3 H NH2 NC(NOH)HCF3 H NH2 NC(NH)NHMeCF3 H NH2 NC(NH)NMe2CF3 H NH2 NC(NH)OMeCF3 H NH2 NC(NH)OEtCF3 Me NH2 NCOMeCF3 Me NH2 NCOEt ¨CF3 Me NH2 NCOPr ¨CF3 Me NH2 NCHO ¨CF3 Me NH2 NCOiPr ¨CF3 Me NH2 NCOtBu ¨CF3 Me NH2 NCOPh ¨CF3 Me NH2 NSO2Me ¨CF3 Me NH2 NSO2Et ¨CF3 Me NH2 NSO2Pr ¨CF3 Me NH2 NSO2PhCF3 Me NH2 NSO2iPrCF3 Me NH2 NNO2CF3 Me NH2 NCOOMeCF3 Me NH2 NCOOEtCF3 Me NH2 NCOOPrCF3 Me NH2 NCOOiPrCF3 Me NH2 NCONHEtCF3 Me NH2 NCONHPrCF3 Me NH2 NCOHCF3 Me NH2 NCONHMeCF3 Me NH2 NCN ¨CF3 Me NH2 NCOSMe ¨CF3 Me NH2 NCOSEtCF3 Me NH2 NCSOMeCF3 Me NH2 NCSOEtCF3 Me NH2 NCSOPrCF3 Me NH2 NSO2HCF3 Me NH2 NSO2NHMeCF3 Me NH2 NSO2NMe2CF3 Me NH2 NP(O)(OMe)2CF3 Me NH2 NP(O)(OEt)2 ¨CF3 Me NH2 NP(O)Me2 ¨CF3 Me NH2 NP(O)Et2 ¨CF3 Me NH2 NP(O)Me(OMe) ¨CF3 Me NH2 NP(O)(OPr)2 ¨CF3 Me NH2 NC(O)C(O)H ¨CF3 Me NH2 NC(O)C(O)Me ¨CF3 Me NH2 NC(O)C(O)OMeCF3 Me NH2 NC(O)C(O)OEtCF3 Me NH2 NC(O)C(O)NH2CF3 Me NH2 NC(O)C(O)OHCF3 Me NH2 NC(NH)HCF3 Me NH2 NC(NOH)HCF3 Me NH2 NC(NH)NHMeCF3 Me NH2 NC(NH)NMe2CF3 Me NH2 NC(NH)OMeCF3 Me NH2 NC(NH)OEtCF3 H H NCOMeCF3 H H NCOEtCF3 H H NCOPrCF3 H H NCHOCF3 H H NCOiPrCF3 H H NCOtBuCF3 H H NCOPhCF3 H H NSO2MeCF3 H H NSO2EtCF3 H H NSO2PrCF3 H H NSO2PhCF3 H H NSO2iPr ¨CF3 H H NNO2 ¨CF3 H H NCOOMe ¨CF3 H H NCOOEt ¨CF3 H H NCOOPr ¨CF3 H H NCOOiPr ¨CF3 H H NCONHEt ¨CF3 H H NCONHPrCF3 H H NCOHCF3 H H NCONHMeCF3 H H NCNCF3 H H NCOSMeCF3 H H NCOSEtCF3 H H NCSOMeCF3 H H NCSOEtCF3 H H NCSOPrCF3 H H NSO2HCF3 H H NSO2NHMeCF3 H H NSO2NMe2CF3 H H NP(O)(OMe)2CF3 H H NP(O)(OEt)2CF3 H H NP(O)Me2CF3 H H NP(O)Et2CF3 H H NP(O)Me(OMe)CF3 H H NP(O)(OPr)2CF3 H H NC(O)C(O)HCF3 H H NC(O)C(O)Me ¨CF3 H H NC(O)C(O)OMe ¨CF3 H H NC(O)C(O)OEt ¨CF3 H H NC(O)C(O)NH2 ¨CF3 H H NC(O)C(O)OH ¨CF3 H H NC(NH)H ¨CF3 H H NC(NOH)H ¨CF3 H H NC(NH)NHMe ¨CF3 H H NC(NH)NMe2 ¨CF3 H H NC(NH)OMe ¨CF3 H H NC(NH)OEtCF3 Me H NCOMeCF3 Me H NCOEtCF3 Me H NCOPrCF3 Me H NCHOCF3 Me H NCOiPrCF3 Me H NCOtBuCF3 Me H NCOPhCF3 Me H NSO2MeCF3 Me H NSO2EtCF3 Me H NSO2PrCF3 Me H NSO2PhCF3 Me H NSO2iPrCF3 Me H NNO2CF3 Me H NCOOMeCF3 Me H NCOOEtCF3 Me H NCOOPrCF3 Me H NCOOiPrCF3 Me H NCONHEt ¨CF3 Me H NCONHPr ¨CF3 Me H NCOH ¨CF3 Me H NCONHMe ¨CF3 Me H NCN ¨CF3 Me H NCOSMe ¨CF3 Me H NCOSEt ¨CF3 Me H NCSOMe ¨CF3 Me H NCSOEt ¨CF3 Me H NCSOPrCF3 Me H NSO2HCF3 Me H NSO2NHMeCF3 Me H NSO2NMe2CF3 Me H NP(O)(OMe)2CF3 Me H NP(O)(OEt)2CF3 Me H NP(O)Me2CF3 Me H NP(O)Et2CF3 Me H NP(O)Me(OMe)CF3 Me H NP(O)(OPr)2CF3 Me H NC(O)C(O)HCF3 Me H NC(O)C(O)MeCF3 Me H NC(O)C(O)OMeCF3 Me H NC(O)C(O)OEtCF3 Me H NC(O)C(O)NH2CF3 Me H NC(O)C(O)OHCF3 Me H NC(NH)HCF3 Me H NC(NOH)HCF3 Me H NC(NH)NHMeCF3 Me H NC(NH)NMe2CF3 Me H NC(NH)OMe ¨CF3 Me H NC(NH)OEt ¨CF3 H Cl NCOMe ¨CF3 H Cl NCOEt ¨CF3 H Cl NCOPr ¨CF3 H Cl NCHO ¨CF3 H Cl NCOiPr ¨CF3 H Cl NCOtBu ¨CF3 H Cl NCOPhCF3 H Cl NSO2MeCF3 H Cl NSO2EtCF3 H Cl NSO2PrCF3 H Cl NSO2PhCF3 H Cl NSO2iPrCF3 H Cl NNO2CF3 H Cl NCOOMeCF3 H Cl NCOOEtCF3 H Cl NCOOPrCF3 H Cl NCOOiPrCF3 H Cl NCONHEtCF3 H Cl NCONHPrCF3 H Cl NCOHCF3 H Cl NCONHMeCF3 H Cl NCNCF3 H Cl NCOSMeCF3 H Cl NCOSEtCF3 H Cl NCSOMeCF3 H Cl NCSOEt ¨CF3 H Cl NCSOPr ¨CF3 H Cl NSO2H ¨CF3 H Cl NSO2NHMe ¨CF3 H Cl NSO2NMe2 ¨CF3 H Cl NP(O)(OMe)2 ¨CF3 H Cl NP(O)(OEt)2 ¨CF3 H Cl NP(O)Me2 ¨CF3 H Cl NP(O)Et2 ¨CF3 H Cl NP(O)Me(OMe) ¨CF3 H Cl NP(O)(OPr)2CF3 H Cl NC(O)C(O)HCF3 H Cl NC(O)C(O)MeCF3 H Cl NC(O)C(O)OMeCF3 H Cl NC(O)C(O)OEtCF3 H Cl NC(O)C(O)NH2CF3 H Cl NC(O)C(O)OHCF3 H Cl NC(NH)HCF3 H Cl NC(NOH)HCF3 H Cl NC(NH)NHMeCF3 H Cl NC(NH)NMe2CF3 H Cl NC(NH)OMeCF3 H Cl NC(NH)OEtCF3 Me Cl NCOMeCF3 Me Cl NCOEtCF3 Me Cl NCOPrCF3 Me Cl NCHOCF3 Me Cl NCOiPrCF3 Me Cl NCOtBuCF3 Me Cl NCOPh ¨CF3 Me Cl NSO2Me ¨CF3 Me Cl NSO2Et ¨CF3 Me Cl NSO2Pr ¨CF3 Me Cl NSO2Ph ¨CF3 Me Cl NSO2iPr ¨CF3 Me Cl NNO2 ¨CF3 Me Cl NCOOMe ¨CF3 Me Cl NCOOEtCF3 Me Cl NCOOPrCF3 Me Cl NCOOiPrCF3 Me Cl NCONHEtCF3 Me Cl NCONHPrCF3 Me Cl NCOHCF3 Me Cl NCONHMeCF3 Me Cl NCNCF3 Me Cl NCOSMeCF3 Me Cl NCOSEtCF3 Me Cl NCSOMeCF3 Me Cl NCSOEtCF3 Me Cl NCSOPrCF3 Me Cl NSO2HCF3 Me Cl NSO2NHMeCF3 Me Cl NSO2NMe2CF3 Me Cl NP(O)(OMe)2CF3 Me Cl NP(O)(OEt)2CF3 Me Cl NP(O)Me2CF3 Me Cl NP(O)Et2 ¨CF3 Me Cl NP(O)Me(OMe) ¨CF3 Me Cl NP(O)(OPr)2 ¨CF3 Me Cl NC(O)C(O)H ¨CF3 Me Cl NC(O)C(O)Me ¨CF3 Me Cl NC(O)C(O)OMe ¨CF3 Me Cl NC(O)C(O)OEt ¨CF3 Me Cl NC(O)C(O)NH2 ¨CF3 Me Cl NC(O)C(O)OH ¨CF3 Me Cl NC(NH)H ¨CF3 Me Cl NC(NOH)H ¨CF3 Me Cl NC(NH)NHMeCF3 Me Cl NC(NH)NMe2CF3 Me Cl NC(NH)OMeCF3 Me Cl NC(NH)OEtMe H NH2 NCOMeMe H NH2 NCOEtMe H NH2 NCOPrMe H NH2 NCHOMe H NH2 NCOiPrMe H NH2 NCOtBuMe H NH2 NCOPhMe H NH2 NSO2MeMe H NH2 NSO2EtMe H NH2 NSO2PrMe H NH2 NSO2PhMe H NH2 NSO2iPrMe H NH2 NNO2 ¨Me H NH2 NCOOMe ¨Me H NH2 NCOOEt ¨Me H NH2 NCOOPr ¨Me H NH2 NCOOiPr ¨Me H NH2 NCONHEt ¨Me H NH2 NCONHPr ¨Me H NH2 NCOH ¨Me H NH2 NCONHMe ¨Me H NH2 NCN ¨Me H NH2 NCOSMe ¨Me H NH2 NCOSEtMe H NH2 NCSOMeMe H NH2 NCSOEtMe H NH2 NCSOPrMe H NH2 NSO2HMe H NH2 NSO2NHMeMe H NH2 NSO2NMe2Me H NH2 NP(O)(OMe)2Me H NH2 NP(O)(OEt)2Me H NH2 NP(O)Me2Me H NH2 NP(O)Et2Me H NH2 NP(O)Me(OMe)Me H NH2 NP(O)(OPr)2Me H NH2 NC(O)C(O)HMe H NH2 NC(O)C(O)MeMe H NH2 NC(O)C(O)OMeMe H NH2 NC(O)C(O)OEtMe H NH2 NC(O)C(O)NH2Me H NH2 NC(O)C(O)OH ¨Me H NH2 NC(NH)H ¨Me H NH2 NC(NOH)H ¨Me H NH2 NC(NH)NHMe ¨Me H NH2 NC(NH)NMe2 ¨Me H NH2 NC(NH)OMe ¨Me H NH2 NC(NH)OEt ¨Me H NH2 NH OMe H NH2 NCOMe OMe H NH2 NCOEt OMe H NH2 NCOPr OMe H NH2 NCHO OMe H NH2 NCOiPr OMe H NH2 NCOtBu OMe H NH2 NCOPh OMe H NH2 NSO2Me OMe H NH2 NSO2Et OMe H NH2 NSO2Pr OMe H NH2 NSO2Ph OMe H NH2 NSO2iPr OMe H NH2 NNO2 OMe H NH2 NCOOMe OMe H NH2 NCOOEt OMe H NH2 NCOOPr OMe H NH2 NCOOiPr OMe H NH2 NCONHEt OMe H NH2 NCONHPr OMe H NH2 NCOH OMe H NH2 NCONHMe OMe H NH2 NCN OMe H NH2 NCOSMe OMe H NH2 NCOSEt OMe H NH2 NCSOMe OMe H NH2 NCSOEt OMe H NH2 NCSOPr OMe H NH2 NSO2H OMe H NH2 NSO2NHMe OMe H NH2 NSO2NMe2 OMe H NH2 NP(O)(OMe)2 OMe H NH2 NP(O)(OEt)2 OMe H NH2 NP(O)Me2 OMe H NH2 NP(O)Et2 OMe H NH2 NP(O)Me(OMe) OMe H NH2 NP(O)(OPr)2 OMe H NH2 NC(O)C(O)H OMe H NH2 NC(O)C(O)Me OMe H NH2 NC(O)C(O)OMe OMe H NH2 NC(O)C(O)OEt OMe H NH2 NC(O)C(O)NH2 OMe H NH2 NC(O)C(O)OH OMe H NH2 NC(NH)H OMe H NH2 NC(NOH)H OMe H NH2 NC(NH)NHMe OMe H NH2 NC(NH)NMe2 OMe H NH2 NC(NH)OMe OMe H NH2 NC(NH)OEt OMe Me NH2 NCOMeMe Me NH2 NCOEt ¨Me Me NH2 NCOPr ¨Me Me NH2 NCHO ¨Me Me NH2 NCOiPr ¨Me Me NH2 NCOtBu ¨Me Me NH2 NCOPh ¨Me Me NH2 NSO2Me ¨Me Me NH2 NSO2Et ¨Me Me NH2 NSO2PrMe Me NH2 NSO2PhMe Me NH2 NSO2iPrMe Me NH2 NNO2Me Me NH2 NCOOMeMe Me NH2 NCOOEtMe Me NH2 NCOOPrMe Me NH2 NCOOiPrMe Me NH2 NCONHEtMe Me NH2 NCONHPrMe Me NH2 NCOHMe Me NH2 NCONHMeMe Me NH2 NCNMe Me NH2 NCOSMeMe Me NH2 NCOSEtMe Me NH2 NCSOMeMe Me NH2 NCSOEtMe Me NH2 NCSOPrMe Me NH2 NSO2HMe Me NH2 NSO2NHMe ¨Me Me NH2 NSO2NMe2 ¨Me Me NH2 NP(O)(OMe)2 ¨Me Me NH2 NP(O)(OEt)2 ¨Me Me NH2 NP(O)Me2 ¨Me Me NH2 NP(O)Et2 ¨Me Me NH2 NP(O)Me(OMe) ¨Me Me NH2 NP(O)(OPr)2 ¨Me Me NH2 NC(O)C(O)H ¨Me Me NH2 NC(O)C(O)Me ¨Me Me NH2 NC(O)C(O)OMeMe Me NH2 NC(O)C(O)OEtMe Me NH2 NC(O)C(O)NH2Me Me NH2 NC(O)C(O)OHMe Me NH2 NC(NH)HMe Me NH2 NC(NOH)HMe Me NH2 NC(NH)NHMeMe Me NH2 NC(NH)NMe2Me Me NH2 NC(NH)OMeMe Me NH2 NC(NH)OEtMe Me NH2 NH OMe Me NH2 NCOMe OMe Me NH2 NCOEt OMe Me NH2 NCOPr OMe Me NH2 NCHO OMe Me NH2 NCOiPr OMe Me NH2 NCOtBu OMe Me NH2 NCOPh OMe Me NH2 NSO2Me OMe Me NH2 NSO2Et OMe Me NH2 NSO2Pr OMe Me NH2 NSO2Ph OMe Me NH2 NSO2iPr OMe Me NH2 NNO2 OMe Me NH2 NCOOMe OMe Me NH2 NCOOEt OMe Me NH2 NCOOPr OMe Me NH2 NCOOiPr OMe Me NH2 NCONHEt OMe Me NH2 NCONHPr OMe Me NH2 NCOH OMe Me NH2 NCONHMe OMe Me NH2 NCN OMe Me NH2 NCOSMe OMe Me NH2 NCOSEt OMe Me NH2 NCSOMe OMe Me NH2 NCSOEt OMe Me NH2 NCSOPr OMe Me NH2 NSO2H OMe Me NH2 NSO2NHMe OMe Me NH2 NSO2NMe2 OMe Me NH2 NP(O)(OMe)2 OMe Me NH2 NP(O)(OEt)2 OMe Me NH2 NP(O)Me2 OMe Me NH2 NP(O)Et2 OMe Me NH2 NP(O)Me(OMe) OMe Me NH2 NP(O)(OPr)2 OMe Me NH2 NC(O)C(O)H OMe Me NH2 NC(O)C(O)Me OMe Me NH2 NC(O)C(O)OMe OMe Me NH2 NC(O)C(O)OEt OMe Me NH2 NC(O)C(O)NH2 OMe Me NH2 NC(O)C(O)OH OMe Me NH2 NC(NH)H OMe Me NH2 NC(NOH)H OMe Me NH2 NC(NH)NHMe OMe Me NH2 NC(NH)NMe2 OMe Me NH2 NC(NH)OMe OMe Me NH2 NC(NH)OEt OMe H H NCOMeMe H H NCOEtMe H H NCOPrMe H H NCHOMe H H NCOiPrMe H H NCOtBuMe H H NCOPhMe H H NSO2MeMe H H NSO2EtMe H H NSO2PrMe H H NSO2PhMe H H NSO2iPrMe H H NNO2Me H H NCOOMeMe H H NCOOEtMe H H NCOOPrMe H H NCOOiPr ¨Me H H NCONHEt ¨Me H H NCONHPr ¨Me H H NCOH ¨Me H H NCONHMe ¨Me H H NCN ¨Me H H NCOSMe ¨Me H H NCOSEt ¨Me H H NCSOMeMe H H NCSOEtMe H H NCSOPrMe H H NSO2HMe H H NSO2NHMeMe H H NSO2NMe2Me H H NP(O)(OMe)2Me H H NP(O)(OEt)2Me H H NP(O)Me2Me H H NP(O)Et2Me H H NP(O)Me(OMe)Me H H NP(O)(OPr)2Me H H NC(O)C(O)HMe H H NC(O)C(O)MeMe H H NC(O)C(O)OMeMe H H NC(O)C(O)OEtMe H H NC(O)C(O)NH2Me H H NC(O)C(O)OHMe H H NC(NH)HMe H H NC(NOH)HMe H H NC(NH)NHMe ¨Me H H NC(NH)NMe2 ¨Me H H NC(NH)OMe ¨Me H H NC(NH)OEt ¨Me H Me NCOMe ¨Me H Me NCOEt ¨Me H Me NCOPr ¨Me H Me NCHO ¨Me H Me NCOiPrMe H Me NCOtBuMe H Me NCOPhMe H Me NSO2MeMe H Me NSO2EtMe H Me NSO2PrMe H Me NSO2PhMe H Me NSO2iPrMe H Me NNO2Me H Me NCOOMeMe H Me NCOOEtMe H Me NCOOPrMe H Me NCOOiPrMe H Me NCONHEtMe H Me NCONHPrMe H Me NCOHMe H Me NCONHMeMe H Me NCNMe H Me NCOSMeMe H Me NCOSEtMe H Me NCSOMe ¨Me H Me NCSOEt ¨Me H Me NCSOPr ¨Me H Me NSO2H ¨Me H Me NSO2NHMe ¨Me H Me NSO2NMe2 ¨Me H Me NP(O)(OMe)2 ¨Me H Me NP(O)(OEt)2 ¨Me H Me NP(O)Me2 ¨Me H Me NP(O)Et2Me H Me NP(O)Me(OMe)Me H Me NP(O)(OPr)2Me H Me NC(O)C(O)HMe H Me NC(O)C(O)MeMe H Me NC(O)C(O)OMe ¨Me H Me NC(O)C(O)OEtMe H Me NC(O)C(O)NH2Me H Me NC(O)C(O)OHMe H Me NC(NH)HMe H Me NC(NOH)H ¨Me H Me NC(NH)NHMe ¨Me H Me NC(NH)NMe2Me H Me NC(NH)OMe ¨Me H Me NC(NH)OEtMe Me Me NCOMeMe Me Me NCOEtMe Me Me NCOPrMe Me Me NCHOMe Me Me NCOiPr ¨Me Me Me NCOtBu ¨Me Me Me NCOPh ¨Me Me Me NSO2Me ¨Me Me Me NSO2Et ¨Me Me Me NSO2Pr ¨Me Me Me NSO2Ph ¨Me Me Me NSO2iPr ¨Me Me Me NNO2Me Me Me NCOOMeMe Me Me NCOOEtMe Me Me NCOOPrMe Me Me NCOOiPrMe Me Me NCONHEtMe Me Me NCONHPrMe Me Me NCOHMe Me Me NCONHMeMe Me Me NCNMe Me Me NCOSMeMe Me Me NCOSEtMe Me Me NCSOMeMe Me Me NCSOEtMe Me Me NCSOPrMe Me Me NSO2HMe Me Me NSO2NHMeMe Me Me NSO2NMe2Me Me Me NP(O)(OMe)2 ¨Me Me Me NP(O)(OEt)2 ¨Me Me Me NP(O)Me2 ¨Me Me Me NP(O)Et2 ¨Me Me Me NP(O)Me(OMe) ¨Me Me Me NP(O)(OPr)2 ¨Me Me Me NC(O)C(O)H ¨Me Me Me NC(O)C(O)Me ¨Me Me Me NC(O)C(O)OMe ¨Me Me Me NC(O)C(O)OEt ¨Me Me Me NC(O)C(O)NH2Me Me Me NC(O)C(O)OHMe Me Me NC(NH)HMe Me Me NC(NOH)HMe Me Me NC(NH)NHMeMe Me Me NC(NH)NMe2Me Me Me NC(NH)OMeMe Me Me NC(NH)OEtMe Me H NCOMeMe Me H NCOEtMe Me H NCOPrMe Me H NCHOMe Me H NCOiPrMe Me H NCOtBuMe Me H NCOPhMe Me H NSO2MeMe Me H NSO2EtMe Me H NSO2PrMe Me H NSO2PhMe Me H NSO2iPrMe Me H NNO2 ¨Me Me H NCOOMe ¨Me Me H NCOOEt ¨Me Me H NCOOPr ¨Me Me H NCOOiPr ¨Me Me H NCONHEt ¨Me Me H NCONHPr ¨Me Me H NCOH ¨Me Me H NCONHMeMe Me H NCNMe Me H NCOSMeMe Me H NCOSEtMe Me H NCSOMeMe Me H NCSOEtMe Me H NCSOPrMe Me H NSO2HMe Me H NSO2NHMeMe Me H NSO2NMe2Me Me H NP(O)(OMe)2Me Me H NP(O)(OEt)2Me Me H NP(O)Me2 ¨Me Me H NP(O)Et2Me Me H NP(O)Me(OMe)Me Me H NP(O)(OPr)2Me Me H NC(O)C(O)HMe Me H NC(O)C(O)MeMe Me H NC(O)C(O)OMeMe Me H NC(O)C(O)OEt ¨Me Me H NC(O)C(O)NH2 ¨Me Me H NC(O)C(O)OH ¨Me Me H NC(NH)H ¨Me Me H NC(NOH)H ¨Me Me H NC(NH)NHMe ¨Me Me H NC(NH)NMe2 ¨Me Me H NC(NH)OMe ¨Me Me H NC(NH)OEt ¨Me CN NH2 NH NHMe CN NHMe NH NHMe CN NMe2 NH NHMe CN NHEt NH NHEt CN NH2 NH NHEt CN NHMe NH NHEt CN NMe2 NH NHEt CN NHEt NH NHCF3 CN NH2 NH NHCF3 CN NHMe NH NHCF3 CN NMe2 NH NHCF3 CN NHEt NH NH
表3R1 R7 R8 NR2 XCF3 CN NH2 NCOMeCF3 CN NH2 NCOEtCF3 CN NH2 NCOPrCF3 CN NH2 NCHOCF3 CN NH2 NCOiPrCF3 CN NH2 NCOtBu ¨CF3 CN NH2 NCOPh ¨CF3 CN NH2 NSO2MeCF3 CN NH2 NSO2EtCF3 CN NH2 NSO2PrCF3 CN NH2 NSO2PhCF3 CN NH2 NSO2iPrCF3 CN NH2 NNO2CF3 CN NH2 NCOOMeCF3 CN NH2 NCOOEt
表3(续)R1 R7 R8 NR2 XCF3 CN NH2 NCOOPr ¨CF3 CN NH2 NCOOiPr ¨CF3 CN NH2 NCONHEt ¨CF3 CN NH2 NCONHPr ¨CF3 CN NH2 NCONH2 ¨CF3 CN NH2 NCONHMe ¨CF3 CN NH2 NCN ¨CF3 CN NH2 NCOSMe ¨CF3 CN NH2 NCOSEtCF3 CN NH2 NCSOMeCF3 CN NH2 NCSOEtCF3 CN NH2 NCSOPrCF3 CN NH2 NSO2NH2CF3 CN NH2 NSO2NHMeCF3 CN NH2 NSO2NMe2CF3 CN NH2 NP(O)(OMe)2CF3 CN NH2 NP(O)(OEt)2CF3 CN NH2 NP(O)Me2CF3 CN NH2 NP(O)Et2CF3 CN NH2 NP(O)Me(OMe)CF3 CN NH2 NP(O)(OPr)2CF3 CN NH2 NC(O)C(O)HCF3 CN NH2 NC(O)C(O)MeCF3 CN NH2 NC(O)C(O)OMeCF3 CN NH2 NC(O)C(O)OEt ¨CF3 CN NH2 NC(O)C(O)NH2 ¨CF3 CN NH2 NC(O)C(O)OH ¨CF3 CN NH2 NC(NH)NH2 ¨CF3 CN NH2 NC(NOH)NH2 ¨CF3 CN NH2 NC(NH)NHMe ¨CF3 CN NH2 NC(NH)NMe2 ¨CF3 CN NH2 NC(NH)OMe ¨CF3 CN NH2 NC(NH)OEt ¨CF3 CN NH2 NH OCF3 CN NH2 NCOMe OCF3 CN NH2 NCOEt OCF3 CN NH2 NCOPr OCF3 CN NH2 NCHO OCF3 CN NH2 NCOiPr OCF3 CN NH2 NCOtBu OCF3 CN NH2 NCOPh OCF3 CN NH2 NSO2Me OCF3 CN NH2 NSO2Et OCF3 CN NH2 NSO2Pr OCF3 CN NH2 NSO2Ph OCF3 CN NH2 NSO2iPr OCF3 CN NH2 NNO2 OCF3 CN NH2 NCOOMe OCF3 CN NH2 NCOOEt OCF3 CN NH2 NCOOPr OCF3 CN NH2 NCOOiPr OCF3 CN NH2 NCONHEt OCF3 CN NH2 NCONHPr OCF3 CN NH2 NCONH2 OCF3 CN NH2 NCONHMe OCF3 CN NH2 NCN OCF3 CN NH2 NCOSMe OCF3 CN NH2 NCOSEt OCF3 CN NH2 NCSOMe OCF3 CN NH2 NCSOEt OCF3 CN NH2 NCSOPr OCF3 CN NH2 NSO2NH2 OCF3 CN NH2 NSO2NHMe OCF3 CN NH2 NSO2NMe2 OCF3 CN NH2 NP(O)(OMe)2 OCF3 CN NH2 NP(O)(OEt)2 OCF3 CN NH2 NP(O)Me2 OCF3 CN NH2 NP(O)Et2 OCF3 CN NH2 NP(O)Me(OMe) OCF3 CN NH2 NP(O)(OPr)2 OCF3 CN NH2 NC(O)C(O)H OCF3 CN NH2 NC(O)C(O)Me OCF3 CN NH2 NC(O)C(O)OMe OCF3 CN NH2 NC(O)C(O)OEt OCF3 CN NH2 NC(O)C(O)NH2 OCF3 CN NH2 NC(O)C(O)OH OCF3 CN NH2 NC(NH)NH2 OCF3 CN NH2 NC(NOH)NH2 OCF3 CN NH2 NC(NH)NHMe OCF3 CN NH2 NC(NH)NMe2 OCF3 CN NH2 NC(NH)OMe OCF3 CN NH2 NC(NH)OEt OCF3 CN H NCOMe ¨CF3 CN H NCOEt ¨CF3 CN H NCOPr ¨CF3 CN H NCHO ¨CF3 CN H NCOiPr ¨CF3 CN H NCOtBu ¨CF3 CN H NCOPh ¨CF3 CN H NSO2Me ¨CF3 CN H NSO2EtCF3 CN H NSO2PrCF3 CN H NSO2PhCF3 CN H NSO2iPrCF3 CN H NNO2CF3 CN H NCOOMeCF3 CN H NCOOEtCF3 CN H NCOOPrCF3 CN H NCOOiPrCF3 CN H NCONHEtCF3 CN H NCONHPrCF3 CN H NCONH2CF3 CN H NCONHMeCF3 CN H NCNCF3 CN H NCOSMeCF3 CN H NCOSEtCF3 CN H NCSOMeCF3 CN H NCSOEtCF3 CN H NCSOPrCF3 CN H NSO2NH2CF3 CN H NSO2NHMe ¨CF3 CN H NSO2NMe2 ¨CF3 CN H NP(O)(OMe)2 ¨CF3 CN H NP(O)(OEt)2 ¨CF3 CN H NP(O)Me2 ¨CF3 CN H NP(O)Et2 ¨CF3 CN H NP(O)Me(OMe) ¨CF3 CN H NP(O)(OPr)2 ¨CF3 CN H NC(O)C(O)HCF3 CN H NC(O)C(O)MeCF3 CN H NC(O)C(O)OMeCF3 CN H NC(O)C(O)OEtCF3 CN H NC(O)C(O)NH2CF3 CN H NC(O)C(O)OHCF3 CN H NC(NH)NH2CF3 CN H NC(NOH)NH2CF3 CN H NC(NH)NHMeCF3 CN H NC(NH)NMe2CF3 CN H NC(NH)OMeCF3 CN H NC(NH)OEtCF3 CN H NH OCF3 CN H NCOMe OCF3 CN H NCOEt OCF3 CN H NCOPr OCF3 CN H NCHO OCF3 CN H NCOiPr OCF3 CN H NCOtBu OCF3 CN H NCOPh OCF3 CN H NSO2Me OCF3 CN H NSO2Et OCF3 CN H NSO2Pr OCF3 CN H NSO2Ph OCF3 CN H NSO2iPr OCF3 CN H NNO2 OCF3 CN H NCOOMe OCF3 CN H NCOOEt OCF3 CN H NCOOPr OCF3 CN H NCOOiFr OCF3 CN H NCONHEt OCF3 CN H NCONHPr OCF3 CN H NCONH2 OCF3 CN H NCONHMe OCF3 CN H NCN OCF3 CN H NCOSMe OCF3 CN H NCOSEt OCF3 CN H NCSOMe OCF3 CN H NCSOEt OCF3 CN H NCSOPr OCF3 CN H NSO2NH2 OCF3 CN H NSO2NHMe OCF3 CN H NSO2NMe2 OCF3 CN H NP(O)(OMe)2 OCF3 CN H NP(O)(OEt)2 OCF3 CN H NP(O)Me2 OCF3 CN H NP(O)Et2 OCF3 CN H NP(O)Me(OMe) OCF3 CN H NP(O)(OPr)2 OCF3 CN H NC(O)C(O)H OCF3 CN H NC(O)C(O)Me OCF3 CN H NC(O)C(O)OMe OCF3 CN H NC(O)C(O)OEt OCF3 CN H NC(O)C(O)NH2 OCF3 CN H NC(O)C(O)OH OCF3 CN H NC(NH)NH2 OCF3 CN H NC(NOH)NH2 OCF3 CN H NC(NH)NHMe OCF3 CN H NC(NH)NMe2 OCF3 CN H NC(NH)OMe OCF3 CN H NC(NH)OEt OCF3 CN SMe NCOMeCF3 CN SMe NCOEtCF3 CN SMe NCOPrCF3 CN SMe NCHOCF3 CN SMe NCOiPrCF3 CN SMe NCOtBuCF3 CN SMe NCOPhCF3 CN SMe NSO2MeCF3 CN SMe NSO2EtCF3 CN SMe NSO2PrCF3 CN SMe NSO2PhCF3 CN SMe NSO2iPrCF3 CN SMe NNO2CF3 CN SMe NCOOMeCF3 CN SMe NCOOEt ¨CF3 CN SMe NCOOPr ¨CF3 CN SMe NCOOiPr ¨CF3 CN SMe NCONHEt ¨CF3 CN SMe NCONHPr ¨CF3 CN SMe NCONH2 ¨CF3 CN SMe NCONHMe ¨CF3 CN SMe NCN ¨CF3 CN SMe NCOSMe ¨CF3 CN SMe NCOSEtCF3 CN SMe NCSOMeCF3 CN SMe NCSOEtCF3 CN SMe NCSOPrCF3 CN SMe NSO2NH2CF3 CN SMe NSO2NHMeCF3 CN SMe NSO2NMe2CF3 CN SMe NP(O)(OMe)2CF3 CN SMe NP(O)(OEt)2CF3 CN SMe NP(O)Me2CF3 CN SMe NP(O)Et2CF3 CN SMe NP(O)Me(OMe) ¨CF3 CN SMe NP(O)(OPr)2CF3 CN SMe NC(O)C(O)HCF3 CN SMe NC(O)C(O)Me ¨CF3 CN SMe NC(O)C(O)OMeCF3 CN SMe NC(O)C(O)OEtCF3 CN SMe NC(O)C(O)NH2 ¨CF3 CN SMe NC(O)C(O)OHCF3 CN SMe NC(NH)NH2CF3 CN SMe NC(NOH)NH2 ¨CF3 CN SMe NC(NH)NHMe ¨CF3 CN SMe NC(NH)NMe2CF3 CN SMe NC(NH)OMe ¨CF3 CN SMe NC(NH)OEt ¨CF3 CN SMe NCOMe OCF3 CN SMe NCOEt OCF3 CN SMe NCOPr OCF3 CN SMe NCHO OCF3 CN SMe NCOiPr OCF3 CN SMe NCOtBu OCF3 CN SMe NCOPh OCF3 CN SMe NSO2Me OCF3 CN SMe NSO2Et OCF3 CN SMe NSO2Pr OCF3 CN SMe NSO2Ph OCF3 CN SMe NSO2iPr OCF3 CN SMe NNO2 OCF3 CN SMe NCOOMe OCF3 CN SMe NCOOEt OCF3 CN SMe NCOOPr OCF3 CN SMe NCOOiPr OCF3 CN SMe NCONHEt OCF3 CN SMe NCONHPr OCF3 CN SMe NCONH2 OCF3 CN SMe NCONHMe OCF3 CN SMe NCN OCF3 CN SMe NCOSMe OCF3 CN SMe NCOSEt OCF3 CN SMe NCSOMe OCF3 CN SMe NCSOEt OCF3 CN SMe NCSOPr OCF3 CN SMe NSO2NH2 OCF3 CN SMe NSO2NHMe OCF3 CN SMe NSO2NMe2 OCF3 CN SMe NP(O)(OMe)2 OCF3 CN SMe NP(O)(OEt)2 OCF3 CN SMe NP(O)Me2 OCF3 CN SMe NP(O)Et2 OCF3 CN SMe NP(O)Me(OMe) OCF3 CN SMe NP(O)(OPr)2 OCF3 CN SMe NC(O)C(O)H OCF3 CN SMe NC(O)C(O)Me OCF3 CN SMe NC(O)C(O)OMe OCF3 CN SMe NC(O)C(O)OEt OCF3 CN SMe NC(O)C(O)NH2 OCF3 CN SMe NC(O)C(O)OH OCF3 CN SMe NC(NH)NH2 OCF3 CN SMe NC(NOH)NH2 OCF3 CN SMe NC(NH)NHMe OCF3 CN SMe NC(NH)NMe2 OCF3 CN SMe NC(NH)OMe OCF3 CN SMe NC(NH)OEt OCF3 CN Cl NCOMeCF3 CN Cl NCOEtCF3 CN Cl NCOPr ¨CF3 CN Cl NCHO ¨CF3 CN Cl NCOiPr ¨CF3 CN Cl NCOtBu ¨CF3 CN Cl NCOPh ¨CF3 CN Cl NSO2Me ¨CF3 CN Cl NSO2Et ¨CF3 CN Cl NSO2Pr ¨CF3 CN Cl NSO2Ph ¨CF3 CN Cl NSO2iPr ¨CF3 CN Cl NNO2CF3 CN Cl NCOOMeCF3 CN Cl NCOOEtCF3 CN Cl NCOOPrCF3 CN Cl NCOOiPrCF3 CN Cl NCONHEtCF3 CN Cl NCONHPrCF3 CN Cl NCONH2CF3 CN Cl NCONHMeCF3 CN Cl NCNCF3 CN Cl NCOSMeCF3 CN Cl NCOSEtCF3 CN Cl NCSOMeCF3 CN Cl NCSOEtCF3 CN Cl NCSOPrCF3 CN Cl NSO2NH2CF3 CN Cl NSO2NHMeCF3 CN Cl NSO2NMe2CF3 CN Cl NP(O)(OMe)2CF3 CN Cl NP(O)(OEt)2 ¨CF3 CN Cl NP(O)Me2 ¨CF3 CN Cl NP(O)Et2 ¨CF3 CN Cl NP(O)Me(OMe) ¨CF3 CN Cl NP(O)(OPr)2 ¨CF3 CN Cl NC(O)C(O)H ¨CF3 CN Cl NC(O)C(O)Me ¨CF3 CN Cl NC(O)C(O)OMeCF3 CN Cl NC(O)C(O)OEtCF3 CN Cl NC(O)C(O)NH2 ¨CF3 CN Cl NC(O)C(O)OHCF3 CN Cl NC(NH)NH2CF3 CN Cl NC(NOH)NH2CF3 CN Cl NC(NH)NHMeCF3 CN Cl NC(NH)NMe2CF3 CN Cl NC(NH)OMeCF3 CN Cl NC(NH)OEtCF3 CN Cl NCOMe OCF3 CN Cl NCOEt OCF3 CN Cl NCOPr OCF3 CN Cl NCHO OCF3 CN Cl NCOiPr OCF3 CN Cl NCOtBu OCF3 CN Cl NCOPh OCF3 CN Cl NSO2Me OCF3 CN Cl NSO2Et OCF3 CN Cl NSO2Pr OCF3 CN Cl NSO2Ph OCF3 CN Cl NSO2iPr OCF3 CN Cl NNO2 OCF3 CN Cl NCOOMe OCF3 CN Cl NCOOEt OCF3 CN Cl NCOOPr OCF3 CN Cl NCOOiPr OCF3 CN Cl NCONHEt OCF3 CN Cl NCONHPr OCF3 CN Cl NCONH2 OCF3 CN Cl NCONHMe OCF3 CN Cl NCN OCF3 CN Cl NCOSMe OCF3 CN Cl NCOSEt OCF3 CN Cl NCSOMe OCF3 CN Cl NCSOEt OCF3 CN Cl NCSOPr OCF3 CN Cl NSO2NH2 OCF3 CN Cl NSO2NHMe OCF3 CN Cl NSO2NMe2 OCF3 CN Cl NP(O)(OMe)2 OCF3 CN Cl NP(O)(OEt)2 OCF3 CN Cl NP(O)Me2 OCF3 CN Cl NP(O)Et2 OCF3 CN Cl NP(O)Me(OMe) OCF3 CN Cl NP(O)(OPr)2 OCF3 CN Cl NC(O)C(O)H OCF3 CN Cl NC(O)C(O)Me OCF3 CN Cl NC(O)C(O)OMe OCF3 CN Cl NC(O)C(O)OEt OCF3 CN Cl NC(O)C(O)NH2 OCF3 CN Cl NC(O)C(O)OH OCF3 CN Cl NC(NH)NH2 OCF3 CN Cl NC(NOH)NH2 OCF3 CN Cl NC(NH)NHMe OCF3 CN Cl NC(NH)NMe2 OCF3 CN Cl NC(NH)OMe OCF3 CN Cl NC(NH)OEt O
表4
R
1 R
9 R
11 NR
2 XCF
3 H H NCOMeCF
3 H H NCOEtCF
3 H H NCOPrCF
3 H H NCHOCF
3 H H NCOiPrCF
3 H H NCOtBuCF
3 H H NCOPhCF
3 H H NSO
2MeCF
3 H H NSO
2EtCF
3 H H NSO
2PrCF
3 H H NSO
2PhCF
3 H H NSO
2iPrCF
3 H H NNO
2CF
3 H H NCOOMe ¨CF
3 H H NCOOEt ¨CF
3 H H NCOOPr ¨
表5(续)R1 R9 R11 NR2 XCF3 H H NCOOiPr ¨CF3 H H NCONHEt ¨CF3 H H NCONHPr ¨CF3 H H NCONH2 ¨CF3 H H NCONHMe ¨CF3 H H NCN ¨CF3 H H NCOSMeCF3 H H NCOSEtCF3 H H NCSOMeCF3 H H NCSOEtCF3 H H NCSOPrCF3 H H NSO2NH2CF3 H H NSO2NHMeCF3 H H NSO2NMe2CF3 H H NP(O)(OMe)2CF3 H H NP(O)(OEt)2CF3 H H NP(O)Me2CF3 H H NP(O)Et2CF3 H H NP(O)Me(OMe)CF3 H H NP(O)(OPr)2CF3 H H NC(O)C(O)HCF3 H H NC(O)C(O)MeCF3 H H NC(O)C(O)OMeCF3 H H NC(O)C(O)OEtCF3 H H NC(O)C(O)NH2 ¨CF3 H H NC(O)C(O)OH ¨CF3 H H NC(NH)NH2 ¨CF3 H H NC(NOH)NH2 ¨CF3 H H NC(NH)NHMe ¨CF3 H H NC(NH)NMe2 ¨CF3 H H NC(NH)OMe ¨CF3 H H NC(NH)OEt ¨CF3 Cl H NCOMe ¨CF3 Cl H NCOEt ¨CF3 Cl H NCOPr ¨CF3 Cl H NCHOCF3 Cl H NCOiPrCF3 Cl H NCOtBuCF3 Cl H NCOPh ¨CF3 Cl H NSO2Me ¨CF3 Cl H NSO2EtCF3 Cl H NSO2Pr ¨CF3 Cl H NSO2Ph ¨CF3 Cl H NSO2iPr ¨CF3 Cl H NNO2 ¨CF3 Cl H NCOOMe ¨CF3 Cl H NCOOEt ¨CF3 Cl H NCOOPr ¨CF3 Cl H NCOOiPr ¨CF3 Cl H NCONHEt ¨CF3 Cl H NCONHPr ¨CF3 Cl H NCONH2 ¨CF3 Cl H NCONHMeCF3 Cl H NCN ¨CF3 Cl H NCOSMe ¨CF3 Cl H NCOSEt ¨CF3 Cl H NCSOMe ¨CF3 Cl H NCSOEt ¨CF3 Cl H NCSOPr ¨CF3 Cl H NSO2NH2 ¨CF3 Cl H NSO2NHMe ¨CF3 Cl H NSO2NMe2 ¨CF3 Cl H NP(O)(OMe)2 ¨CF3 Cl H NP(O)(OEt)2 ¨CF3 Cl H NP(O)Me2CF3 Cl H NP(O)Et2CF3 Cl H NP(O)Me(OMe)CF3 Cl H NP(O)(OPr)2CF3 Cl H NC(O)C(O)HCF3 Cl H NC(O)C(O)MeCF3 Cl H NC(O)C(O)OMeCF3 Cl H NC(O)C(O)OEtCF3 Cl H NC(O)C(O)NH2 ¨CF3 Cl H NC(O)C(O)OHCF3 Cl H NC(NH)NH2 ¨CF3 Cl H NC(NOH)NH2 ¨CF3 Cl H NC(NH)NHMeCF3 Cl H NC(NH)NMe2CF3 Cl H NC(NH)OMeCF3 Cl H NC(NH)OEtCF3 Cl Me NCOMe ¨CF3 Cl Me NCOEt ¨CF3 Cl Me NCOPr ¨CF3 Cl Me NCHO ¨CF3 Cl Me NCOiPr ¨CF3 Cl Me NCOtBu ¨CF3 Cl Me NCOPh ¨CF3 Cl Me NSO2Me ¨CF3 Cl Me NSO2Et ¨CF3 Cl Me NSO2Pr ¨CF3 Cl Me NSO2PhCF3 Cl Me NSO2iPrCF3 Cl Me NNO2CF3 Cl Me NCOOMeCF3 Cl Me NCOOEtCF3 Cl Me NCOOPrCF3 Cl Me NCOOiPrCF3 Cl Me NCONHEtCF3 Cl Me NCONHPrCF3 Cl Me NCONH2CF3 Cl Me NCONHMeCF3 Cl Me NCNCF3 Cl Me NCOSMeCF3 Cl Me NCOSEtCF3 Cl Me NCSOMeCF3 Cl Me NCSOEtCF3 Cl Me NCSOPrCF3 Cl Me NSO2NH2CF3 Cl Me NSO2NHMeCF3 Cl Me NSO2NMe2 ¨CF3 Cl Me NP(O)(OMe)2 ¨CF3 Cl Me NP(O)(OEt)2 ¨CF3 Cl Me NP(O)Me2 ¨CF3 Cl Me NP(O)Et2 ¨CF3 Cl Me NP(O)Me(OMe) ¨CF3 Cl Me NP(O)(OPr)2 ¨CF3 Cl Me NC(O)C(O)H ¨CF3 Cl Me NC(O)C(O)Me ¨CF3 Cl Me NC(O)C(O)OMe ¨CF3 Cl Me NC(O)C(O)OEtCF3 Cl Me NC(O)C(O)NH2CF3 Cl Me NC(O)C(O)OHCF3 Cl Me NC(NH)NH2CF3 Cl Me NC(NOH)NH2CF3 Cl Me NC(NH)NHMeCF3 Cl Me NC(NH)NMe2CF3 Cl Me NC(NH)OMeCF3 Cl Me NC(NH)OEtCF3 Cl SMe NCOMeCF3 Cl SMe NCOEtCF3 Cl SMe NCOPrCF3 Cl SMe NCHOCF3 Cl SMe NCOiPrCF3 Cl SMe NCOtBu ¨CF3 Cl SMe NCOPhCF3 Cl SMe NSO2Me ¨CF3 Cl SMe NSO2EtCF3 Cl SMe NSO2Pr ¨CF3 Cl SMe NSO2Ph ¨CF3 Cl SMe NSO2iPr ¨CF3 Cl SMe NNO2 ¨CF3 Cl SMe NCOOMe ¨CF3 Cl SMe NCOOEt ¨CF3 Cl SMe NCOOPr ¨CF3 Cl SMe NCOOiPr ¨CF3 Cl SMe NCONHEt ¨CF3 Cl SMe NCONHPr ¨CF3 Cl SMe NCONH2CF3 Cl SMe NCONHMeCF3 Cl SMe NCNCF3 Cl SMe NCOSMeCF3 Cl SMe NCOSEtCF3 Cl SMe NCSOMeCF3 Cl SMe NCSOEtCF3 Cl SMe NCSOPrCF3 Cl SMe NSO2NH2CF3 Cl SMe NSO2NHMeCF3 Cl SMe NSO2NMe2CF3 Cl SMe NP(O)(OMe)2CF3 Cl SMe NP(O)(OEt)2CF3 Cl SMe NP(O)Me2CF3 Cl SMe NP(O)Et2CF3 Cl SMe NP(O)Me(OMe)CF3 Cl SMe NP(O)(OPr)2CF3 Cl SMe NC(O)C(O)H ¨CF3 Cl SMe NC(O)C(O)Me ¨CF3 Cl SMe NC(O)C(O)OMe ¨CF3 Cl SMe NC(O)C(O)OEt ¨CF3 Cl SMe NC(O)C(O)NH2 ¨CF3 Cl SMe NC(O)C(O)OH ¨CF3 Cl SMe NC(NH)NH2 ¨CF3 Cl SMe NC(NOH)NH2 ¨CF3 Cl SMe NC(NH)NHMe ¨CF3 Cl SMe NC(NH)NMe2 ¨CF3 Cl SMe NC(NH)OMe ¨CF3 Cl SMe NC(NH)OEt ¨CF3 H Me NCOMe ¨CF3 H Me NCOEt ¨CF3 H Me NCOPr ¨CF3 H Me NCHOCF3 H Me NCOiPr ¨CF3 H Me NCOtBu ¨CF3 H Me NCOPh ¨CF3 H Me NSO2Me ¨CF3 H Me NSO2EtCF3 H Me NSO2Pr ¨CF3 H Me NSO2PhCF3 H Me NSO2iPrCF3 H Me NNO2CF3 H Me NCOOMe ¨CF3 H Me NCOOEtCF3 H Me NCOOPrCF3 H Me NCOOiPrCF3 H Me NCONHEt ¨CF3 H Me NCONHPr ¨CF3 H Me NCONH2 ¨CF3 H Me NCONHMe ¨CF3 H Me NCN ¨CF3 H Me NCOSMe ¨CF3 H Me NCOSEt ¨CF3 H Me NCSOMeCF3 H Me NCSOEtCF3 H Me NCSOPrCF3 H Me NSO2NH2CF3 H Me NSO2NHMeCF3 H Me NSO2NMe2CF3 H Me NP(O)(OMe)2CF3 H Me NP(O)(OEt)2CF3 H Me NP(O)Me2CF3 H Me NP(O)Et2CF3 H Me NP(O)Me(OMe)CF3 H Me NP(O)(OPr)2CF3 H Me NC(O)C(O)HCF3 H Me NC(O)C(O)MeCF3 H Me NC(O)C(O)OMeCF3 H Me NC(O)C(O)OEtCF3 H Me NC(O)C(O)NH2CF3 H Me NC(O)C(O)OHCF3 H Me NC(NH)NH2CF3 H Me NC(NOH)NH2CF3 H Me NC(NH)NHMeCF3 H Me NC(NH)NMe2 ¨CF3 H Me NC(NH)OMe ¨CF3 H Me NC(NH)OEt ¨CF3 H SMe NCOMe ¨CF3 H SMe NCOEt ¨CF3 H SMe NCOPr ¨CF3 H SMe NCHO ¨CF3 H SMe NCOiPr ¨CF3 H SMe NCOtBu ¨CF3 H SMe NCOPh ¨CF3 H SMe NSO2MeCF3 H SMe NSO2EtCF3 H SMe NSO2PrCF3 H SMe NSO2PhCF3 H SMe NSO2iPrCF3 H SMe NNO2CF3 H SMe NCOOMeCF3 H SMe NCOOEtCF3 H SMe NCOOPrCF3 H SMe NCOOiPrCF3 H SMe NCONHEtCF3 H SMe NCONHPrCF3 H SMe NCONH2CF3 H SMe NCONHMe ¨CF3 H SMe NCNCF3 H SMe NCOSMeCF3 H SMe NCOSEtCF3 H SMe NCSOMeCF3 H SMe NCSOEt ¨CF3 H SMe NCSOPr ¨CF3 H SMe NSO2NH2 ¨CF3 H SMe NSO2NHMe ¨CF3 H SMe NSO2NMe2 ¨CF3 H SMe NP(O)(OMe)2 ¨CF3 H SMe NP(O)(OEt)2 ¨CF3 H SMe NP(O)Me2 ¨CF3 H SMe NP(O)Et2 ¨CF3 H SMe NP(O)Me(OMe)CF3 H SMe NP(O)(OPr)2CF3 H SMe NC(O)C(O)HCF3 H SMe NC(O)C(O)Me ¨CF3 H SMe NC(O)C(O)OMeCF3 H SMe NC(O)C(O)OEtCF3 H SMe NC(O)C(O)NH2CF3 H SMe NC(O)C(O)OHCF3 H SMe NC(NH)NH2 ¨CF3 H SMe NC(NOH)NH2 ¨CF3 H SMe NC(NH)NHMe ¨CF3 H SMe NC(NH)NMe2 ¨CF3 H SMe NC(NH)OMe ¨CF3 H SMe NC(NH)OEtCF3 Me H NCOMeCF3 Me H NCOEt ¨CF3 Me H NCOPr ¨CF3 Me H NCHO ¨CF3 Me H NCOiPrCF3 Me H NCOtBuCF3 Me H NCOPhCF3 Me H NSO2MeCF3 Me H NSO2EtCF3 Me H NSO2PrCF3 Me H NSO2PhCF3 Me H NSO2iPrCF3 Me H NNO2CF3 Me H NCOOMeCF3 Me H NCOOEtCF3 Me H NCOOPrCF3 Me H NCOOiPrCF3 Me H NCONHEtCF3 Me H NCONHPrCF3 Me H NCONH2CF3 Me H NCONHMeCF3 Me H NCNCF3 Me H NCOSMeCF3 Me H NCOSEtCF3 Me H NCSOMeCF3 Me H NCSOEtCF3 Me H NCSOPrCF3 Me H NSO2NH2CF3 Me H NSO2NHMeCF3 Me H NSO2NMe2CF3 Me H NP(O)(OMe)2CF3 Me H NP(O)(OEt)2CF3 Me H NP(O)Me2CF3 Me H NP(O)Et2CF3 Me H NP(O)Me(OMe) ¨CF3 Me H NP(O)(OPr)2 ¨CF3 Me H NC(O)C(O)H ¨CF3 Me H NC(O)C(O)Me ¨CF3 Me H NC(O)C(O)OMe ¨CF3 Me H NC(O)C(O)OEt ¨CF3 Me H NC(O)C(O)NH2 ¨CF3 Me H NC(O)C(O)OH ¨CF3 Me H NC(NH)NH2CF3 Me H NC(NOH)NH2CF3 Me H NC(NH)NHMe ¨CF3 Me H NC(NH)NMe2CF3 Me H NC(NH)OMeCF3 Me H NC(NH)OEtCF3 Me Me NCOMeCF3 Me Me NCOEtCF3 Me Me NCOPrCF3 Me Me NCHOCF3 Me Me NCOiPr ¨CF3 Me Me NCOtBuCF3 Me Me NCOPh ¨CF3 Me Me NSO2MeCF3 Me Me NSO2EtCF3 Me Me NSO2Pr ¨CF3 Me Me NSO2PhCF3 Me Me NSO2iPrCF3 Me Me NNO2CF3 Me Me NCOOMe ¨CF3 Me Me NCOOEt ¨CF3 Me Me NCOOPr ¨CF3 Me Me NCOOiPr ¨CF3 Me Me NCONHEt ¨CF3 Me Me NCONHPr ¨CF3 Me Me NCONH2 ¨CF3 Me Me NCONHMe ¨CF3 Me Me NCN ¨CF3 Me Me NCOSMe ¨CF3 Me Me NCOSEtCF3 Me Me NCSOMeCF3 Me Me NCSOEt ¨CF3 Me Me NCSOPr ¨CF3 Me Me NSO2NH2 ¨CF3 Me Me NSO2NHMe ¨CF3 Me Me NSO2NMe2 ¨CF3 Me Me NP(O)(OMe)2 ¨CF3 Me Me NP(O)(OEt)2CF3 Me Me NP(O)Me2CF3 Me Me NP(O)Et2 ¨CF3 Me Me NP(O)Me(OMe) ¨CF3 Me Me NP(O)(OPr)2 ¨CF3 Me Me NC(O)C(O)HCF3 Me Me NC(O)C(O)Me ¨CF3 Me Me NC(O)C(O)OMe ¨CF3 Me Me NC(O)C(O)OEt ¨CF3 Me Me NC(O)C(O)NH2 ¨CF3 Me Me NC(O)C(O)OH ¨CF3 Me Me NC(NH)NH2 ¨CF3 Me Me NC(NOH)NH2 ¨CF3 Me Me NC(NH)NHMe ¨CF3 Me Me NC(NH)NMe2 ¨CF3 Me Me NC(NH)OMe ¨CF3 Me Me NC(NH)OEt ¨Me H H NCOMe ¨Me H H NCOEt ¨Me H H NCOPrMe H H NCHOMe H H NCOiPrMe H H NCOtBuMe H H NCOPhMe H H NSO2MeMe H H NSO2EtMe H H NSO2PrMe H H NSO2PhMe H H NSO2iPrMe H H NNO2Me H H NCOOMeMe H H NCOOEtMe H H NCOOPrMe H H NCOOiPrMe H H NCONHEtMe H H NCONHPrMe H H NCONH2Me H H NCONHMeMe H H NCNMe H H NCOSMe ¨Me H H NCOSEt ¨Me H H NCSOMe ¨Me H H NCSOEt ¨Me H H NCSOPr ¨Me H H NSO2NH2 ¨Me H H NSO2NHMe ¨Me H H NSO2NMe2 ¨Me H H NP(O)(OMe)2 ¨Me H H NP(O)(OEt)2 ¨Me H H NP(O)Me2Me H H NP(O)Et2 ¨Me H H NP(O)Me(OMe)Me H H NP(O)(OPr)2 ¨Me H H NC(O)C(O)H ¨Me H H NC(O)C(O)MeMe H H NC(O)C(O)OMeMe H H NC(O)C(O)OEtMe H H NC(O)C(O)NH2Me H H NC(O)C(O)OHMe H H NC(NH)NH2Me H H NC(NOH)NH2Me H H NC(NH)NHMeMe H H NC(NH)NMe2Me H H NC(NH)OMeMe H H NC(NH)OEt ¨Me Cl H NCOMeMe Cl H NCOEt ¨Me Cl H NCOPr ¨Me Cl H NCHO ¨Me Cl H NCOiPr ¨Me Cl H NCOtBu ¨Me Cl H NCOPh ¨Me Cl H NSO2Me ¨Me Cl H NSO2Et ¨Me Cl H NSO2Pr ¨Me Cl H NSO2Ph ¨Me Cl H NSO2iPr ¨Me Cl H NNO2Me Cl H NCOOMeMe Cl H NCOOEtMe Cl H NCOOPrMe Cl H NCOOiPr ¨Me Cl H NCONHEtMe Cl H NCONHPrMe Cl H NCONH2Me Cl H NCONHMe ¨Me Cl H NCN ¨Me Cl H NCOSMe ¨Me Cl H NCOSEt ¨Me Cl H NCSOMe ¨Me Cl H NCSOEt ¨Me Cl H NCSOPrMe Cl H NSO2NH2 ¨Me Cl H NSO2NHMeMe Cl H NSO2NMe2Me Cl H NP(O)(OMe)2 ¨Me Cl H NP(O)(OEt)2 ¨Me Cl H NP(O)Me2 ¨Me Cl H NP(O)Et2 ¨Me Cl H NP(O)Me(OMe) ¨Me Cl H NP(O)(OPr)2 ¨Me Cl H NC(O)C(O)H ¨Me Cl H NC(O)C(O)Me ¨Me Cl H NC(O)C(O)OMe ¨Me Cl H NC(O)C(O)OEt ¨Me Cl H NC(O)C(O)NH2Me Cl H NC(O)C(O)OH ¨Me Cl H NC(NH)NH2Me Cl H NC(NOH)NH2Me Cl H NC(NH)NHMeMe Cl H NC(NH)NMe2 ¨Me Cl H NC(NH)OMeMe Cl H NC(NH)OEtMe Cl Me NCOMe ¨Me Cl Me NCOEtMe Cl Me NCOPr ¨Me Cl Me NCHO ¨Me Cl Me NCOiPr ¨Me Cl Me NCOtBuMe Cl Me NCOPhMe Cl Me NSO2MeMe Cl Me NSO2EtMe Cl Me NSO2PrMe Cl Me NSO2Ph ¨Me Cl Me NSO2iPr ¨Me Cl Me NNO2 ¨Me Cl Me NCOOMe ¨Me Cl Me NCOOEt ¨Me Cl Me NCOOPr ¨Me Cl Me NCOOiPr ¨Me Cl Me NCONHEt ¨Me Cl Me NCONHPr ¨Me Cl Me NCONH2 ¨Me Cl Me NCONHMe ¨Me Cl Me NCN ¨Me Cl Me NCOSMe ¨Me Cl Me NCOSEt ¨Me Cl Me NCSOMeMe Cl Me NCSOEtMe Cl Me NCSOPr ¨Me Cl Me NSO2NH2 ¨Me Cl Me NSO2NHMe ¨Me Cl Me NSO2NMe2 ¨Me Cl Me NP(O)(OMe)2 ¨Me Cl Me NP(O)(OEt)2 ¨Me Cl Me NP(O)Me2 ¨Me Ci Me NP(O)Et2 ¨Me Cl Me NP(O)Me(OMe) ¨Me Cl Me NP(O)(OPr)2 ¨Me Cl Me NC(O)C(O)HMe Cl Me NC(O)C(O)Me ¨Me Cl Me NC(O)C(O)OMe ¨Me Cl Me NC(O)C(O)OEt ¨Me Cl Me NC(O)C(O)NH2 ¨Me Cl Me NC(O)C(O)OH ¨Me Cl Me NC(NH)NH2 ¨Me Cl Me NC(NOH)NH2 ¨Me Cl Me NC(NH)NHMe ¨Me Cl Me NC(NH)NMe2 ¨Me Cl Me NC(NH)OMe ¨Me Cl Me NC(NH)OEtMe Cl SMe NCOMeMe Cl SMe NCOEt ¨Me Cl SMe NCOPrMe Cl SMe NCHOMe Cl SMe NCOiPrMe Cl SMe NCOtBuMe Cl SMe NCOPhMe Cl SMe NSO2Me ¨Me Cl SMe NSO2EtMe Cl SMe NSO2PrMe Cl SMe NSO2Ph ¨Me Cl SMe NSO2iPrMe Cl SMe NNO2Me Cl SMe NCOOMeMe Cl SMe NCOOEtMe Cl SMe NCOOPrMe Cl SMe NCOOiPrMe Cl SMe NCONHEt ¨Me Cl SMe NCONHPr ¨Me Cl SMe NCONH2 ¨Me Cl SMe NCONHMe ¨Me Cl SMe NCN ¨Me Cl SMe NCOSMe ¨Me Cl SMe NCOSEt ¨Me Cl SMe NCSOMe ¨Me Cl SMe NCSOEt ¨Me Cl SMe NCSOPr ¨Me Cl SMe NSO2NH2 ¨Me Cl SMe NSO2NHMeMe Cl SMe NSO2NMe2Me Cl SMe NP(O)(OMe)2Me Cl SMe NP(O)(OEt)2Me Cl SMe NP(O)Me2Me Cl SMe NP(O)Et2Me Cl SMe NP(O)Me(OMe) ¨Me Cl SMe NP(O)(OPr)2 ¨Me Cl SMe NC(O)C(O)H ¨Me Cl SMe NC(O)C(O)MeMe Cl SMe NC(O)C(O)OMe ¨Me Cl SMe NC(O)C(O)OEt ¨Me Cl SMe NC(O)C(O)NH2 ¨Me Cl SMe NC(O)C(O)OH ¨Me Cl SMe NC(NH)NH2Me Cl SMe NC(NOH)NH2 ¨Me Cl SMe NC(NH)NHMeMe Cl SMe NC(NH)NMe2 ¨Me Cl SMe NC(NH)OMe ¨Me Cl SMe NC(NH)OEt ¨Me H Me NCOMe ¨Me H Me NCOEt ¨Me H Me NCOPr ¨Me H Me NCHO ¨Me H Me NCOiPr ¨Me H Me NCOtBu ¨Me H Me NCOPh ¨Me H Me NSO2MeMe H Me NSO2Et ¨Me H Me NSO2PrMe H Me NSO2PhMe H Me NSO2iPrMe H Me NNO2Me H Me NCOOMeMe H Me NCOOEtMe H Me NCOOPrMe H Me NCOOiPr ¨Me H Me NCONHEt ¨Me H Me NCONHPrMe H Me NCONH2Me H Me NCONHMeMe H Me NCNMe H Me NCOSMeMe H Me NCOSEtMe H Me NCSOMeMe H Me NCSOEt ¨Me H Me NCSOPr ¨Me H Me NSO2NH2 ¨Me H Me NSO2NHMe ¨Me H Me NSO2NMe2 ¨Me H Me NP(O)(OMe)2 ¨Me H Me NP(O)(OEt)2 ¨Me H Me NP(O)Me2 ¨Me H Me NP(O)Et2 ¨Me H Me NP(O)Me(OMe)Me H Me NP(O)(OPr)2Me H Me NC(O)C(O)HMe H Me NC(O)C(O)MeMe H Me NC(O)C(O)OMeMe H Me NC(O)C(O)OEtMe H Me NC(O)C(O)NH2Me H Me NC(O)C(O)OHMe H Me NC(NH)NH2Me H Me NC(NOH)NH2Me H Me NC(NH)NHMeMe H Me NC(NH)NMe2Me H Me NC(NH)OMeMe H Me NC(NH)OEtMe H SMe NCOMeMe H SMe NCOEtMe H SMe NCOPrMe H SMe NCHOMe H SMe NCOiPrMe H SMe NCOtBu ¨Me H SMe NCOPh ¨Me H SMe NSO2Me ¨Me H SMe NSO2Et ¨Me H SMe NSO2Pr ¨Me H SMe NSO2Ph ¨Me H SMe NSO2iPr ¨Me H SMe NNO2 ¨Me H SMe NCOOMe ¨Me H SMe NCOOEt ¨Me H SMe NCOOPr ¨Me H SMe NCOOiPrMe H SMe NCONHEt ¨Me H SMe NCONHPr ¨Me H SMe NCONH2Me H SMe NCONHMeMe H SMe NCNMe H SMe NCOSMe ¨Me H SMe NCOSEtMe H SMe NCSOMe ¨Me H SMe NCSOEt ¨Me H SMe NCSOPr ¨Me H SMe NSO2NH2 ¨Me H SMe NSO2NHMe ¨Me H SMe NSO2NMe2 ¨Me H SMe NP(O)(OMe)2Me H SMe NP(O)(OEt)2 ¨Me H SMe NP(O)Me2Me H SMe NP(O)Et2 ¨Me H SMe NP(O)Me(OMe) ¨Me H SMe NP(O)(OPr)2 ¨Me H SMe NC(O)C(O)H ¨Me H SMe NC(O)C(O)Me ¨Me H SMe NC(O)C(O)OMe ¨Me H SMe NC(O)C(O)OEt ¨Me H SMe NC(O)C(O)NH2 ¨Me H SMe NC(O)C(O)OH ¨Me H SMe NC(NH)NH2 ¨Me H SMe NC(NOH)NH2Me H SMe NC(NH)NHMeMe H SMe NC(NH)NMe2Me H SMe NC(NH)OMeMe H SMe NC(NH)OEtMe Me H NCOMeMe Me H NCOEtMe Me H NCOPrMe Me H NCHOMe Me H NCOiPrMe Me H NCOtBuMe Me H NCOPh ¨Me Me H NSO2MeMe Me H NSO2EtMe Me H NSO2PrMe Me H NSO2PhMe Me H NSO2iPrMe Me H NNO2Me Me H NCOOMeMe Me H NCOOEt ¨Me Me H NCOOPr ¨Me Me H NCOOiPr ¨Me Me H NCONHEt ¨Me Me H NCONHPr ¨Me Me H NCONH2 ¨Me Me H NCONHMe ¨Me Me H NCN ¨Me Me H NCOSMeMe Me H NCOSEtMe Me H NCSOMeMe Me H NCSOEtMe Me H NCSOPrMe Me H NSO2NH2Me Me H NSO2NHMeMe Me H NSO2NMe2Me Me H NP(O)(OMe)2Me Me H NP(O)(OEt)2Me Me H NP(O)Me2Me Me H NP(O)Et2Me Me H NP(O)Me(OMe)Me Me H NP(O)(OPr)2Me Me H NC(O)C(O)HMe Me H NC(O)C(O)MeMe Me H NC(O)C(O)OMeMe Me H NC(O)C(O)OEtMe Me H NC(O)C(O)NH2Me Me H NC(O)C(O)OH ¨Me Me H NC(NH)NH2 ¨Me Me H NC(NOH)NH2 ¨Me Me H NC(NH)NHMe ¨Me Me H NC(NH)NMe2 ¨Me Me H NC(NH)OMe ¨Me Me H NC(NH)OEt ¨Me Me Me NCOMe ¨Me Me Me NCOEt ¨Me Me Me NCOPr ¨Me Me Me NCHOMe Me Me NCOiPrMe Me Me NCOtBuMe Me Me NCOPhMe Me Me NSO2MeMe Me Me NSO2EtMe Me Me NSO2PrMe Me Me NSO2PhMe Me Me NSO2iPrMe Me Me NNO2 ¨Me Me Me NCOOMe ¨Me Me Me NCOOEt ¨Me Me Me NCOOPrMe Me Me NCOOiPr ¨Me Me Me NCONHEt ¨Me Me Me NCONHPr ¨Me Me Me NCONH2Me Me Me NCONHMeMe Me Me NCNMe Me Me NCOSMeMe Me Me NCOSEtMe Me Me NCSOMeMe Me Me NCSOEtMe Me Me NCSOPrMe Me Me NSO2NH2Me Me Me NSO2NHMeMe Me Me NSO2NMe2Me Me Me NP(O)(OMe)2Me Me Me NP(O)(OEt)2Me Me Me NP(O)Me2Me Me Me NP(O)Et2Me Me Me NP(O)Me(OMe)Me Me Me NP(O)(OPr)2Me Me Me NC(O)C(O)HMe Me Me NC(O)C(O)MeMe Me Me NC(O)C(O)OMeMe Me Me NC(O)C(O)OEtMe Me Me NC(O)C(O)NH2Me Me Me NC(O)C(O)OHMe Me Me NC(NH)NH2Me Me Me NC(NOH)NH2Me Me Me NC(NH)NHMeMe Me Me NC(NH)NMe2Me Me Me NC(NH)OMeMe Me Me NC(NH)OEt
表5R1 R12 R13 NR2 XCF3 Cl Me NCOMeCF3 Cl Me NCOEtCF3 Cl Me NCOPrCF3 Cl Me NCHOCF3 Cl Me NCOiPrCF3 Cl Me NCOtBuCF3 Cl Me NCOPhCF3 Cl Me NSO2MeCF3 Cl Me NSO2EtCF3 Cl Me NSO2PrCF3 Cl Me NSO2PhCF3 Cl Me NSO2iPrCF3 Cl Me NNO2CF3 Cl Me NCOOMe ¨CF3 Cl Me NCOOEt ¨CF3 Cl Me NCOOPr ¨CF3 Cl Me NCOOiPr ¨
表5(续)R1 R12 R13 NR2 XCF3 Cl Me NCONHEt ¨CF3 Cl Me NCONHPr ¨CF3 Cl Me NCONH2 ¨CF3 Cl Me NCONHMe ¨CF3 Cl Me NCN ¨CF3 Cl Me NCOSMe ¨CF3 Cl Me NCOSEt ¨CF3 Cl Me NCSOMeCF3 Cl Me NCSOEtCF3 Cl Me NCSOPrCF3 Cl Me NSO2NH2CF3 Cl Me NSO2NHMeCF3 Cl Me NSO2NMe2 ¨CF3 Cl Me NP(O)(OMe)2CF3 Cl Me NP(O)(OEt)2CF3 Cl Me NP(O)Me2CF3 Cl Me NP(O)Et2 ¨CF3 Ci Me NP(O)Me(OMe) ¨CF3 Cl Me NP(O)(OPr)2 ¨CF3 Cl Me NC(O)C(O)H ¨CF3 Cl Me NC(O)C(O)Me ¨CF3 Cl Me NC(O)C(O)OMe ¨CF3 Cl Me NC(O)C(O)OEt ¨CF3 Cl Me NC(O)C(O)NH2CF3 Cl Me NC(O)C(O)OH ¨CF3 Cl Me NC(NH)NH2 ¨CF3 Cl Me NC(NOH)NH2 ¨CF3 Cl Me NC(NH)NHMe ¨CF3 Cl Me NC(NH)NMe2 ¨CF3 Cl Me NC(NH)OMe ¨CF3 Cl Me NC(NH)OEt ¨CF3 Cl Me NCOMe OCF3 Cl Me NCOEt OCF3 Cl Me NCOPr OCF3 Cl Me NCHO OCF3 Cl Me NCOiPr OCF3 Cl Me NCOtBu OCF3 Cl Me NCOPh OCF3 Cl Me NSO2Me OCF3 Cl Me NSO2Et OCF3 Cl Me NSO2Pr OCF3 Cl Me NSO2Ph OCF3 Cl Me NSO2iPr OCF3 Cl Me NNO2 OCF3 Cl Me NCOOMe OCF3 Cl Me NCOOEt OCF3 Cl Me NCOOPr OCF3 Cl Me NCOOiPr OCF3 Cl Me NCONHEt OCF3 Cl Me NCONHPr OCF3 Cl Me NCONH2 OCF3 Cl Me NCONHMe OCF3 Cl Me NCN OCF3 Cl Me NCOSMe OCF3 Cl Me NCOSEt OCF3 Cl Me NCSOMe OCF3 Cl Me NCSOEt OCF3 Cl Me NCSOPr OCF3 Cl Me NSO2NH2 OCF3 Cl Me NSO2NHMe OCF3 Cl Me NSO2NMe2 OCF3 Cl Me NP(O)(OMe)2 OCF3 Cl Me NP(O)(OEt)2 OCF3 Cl Me NP(O)Me2 OCF3 Cl Me NP(O)Et2 OCF3 Cl Me NP(O)Me(OMe) OCF3 Cl Me NP(O)(OPr)2 OCF3 Cl Me NC(O)C(O)H OCF3 Cl Me NC(O)C(O)Me OCF3 Cl Me NC(O)C(O)OMe OCF3 Cl Me NC(O)C(O)OEt OCF3 Cl Me NC(O)C(O)NH2 OCF3 Cl Me NC(O)C(O)OH OCF3 Cl Me NC(NH)NH2 OCF3 Cl Me NC(NOH)NH2 OCF3 Cl Me NC(NH)NHMe OCF3 Cl Me NC(NH)NMe2 OCF3 Cl Me NC(NH)OMe OCF3 Cl Me NC(NH)OEt OCF3 H Me NCOMe ¨CF3 H Me NCOEt ¨CF3 H Me NCOPr ¨CF3 H Me NCHO ¨CF3 H Me NCOiPr ¨CF3 H Me NCOtBu ¨CF3 H Me NCOPh ¨CF3 H Me NSO2Me ¨CF3 H Me NSO2Et ¨CF3 H Me NSO2Pr ¨CF3 H Me NSO2Ph ¨CF3 H Me NSO2iPr ¨CF3 H Me NNO2CF3 H Me NCOOMeCF3 H Me NCOOEtCF3 H Me NCOOPr ¨CF3 H Me NCOOiPrCF3 H Me NCONHEtCF3 H Me NCONHPrCF3 H Me NCONH2 ¨CF3 H Me NCONHMe ¨CF3 H Me NCN ¨CF3 H Me NCOSMe ¨CF3 H Me NCOSEt ¨CF3 H Me NCSOMe ¨CF3 H Me NCSOEt ¨CF3 H Me NCSOPr ¨CF3 H Me NSO2NH2 ¨CF3 H Me NSO2NHMeCF3 H Me NSO2NMe2CF3 H Me NP(O)(OMe)2 ¨CF3 H Me NP(O)(OEt)2 ¨CF3 H Me NP(O)Me2 ¨CF3 H Me NP(O)Et2 ¨CF3 H Me NP(O)Me(OMe) ¨CF3 H Me NP(O)(OPr)2 ¨CF3 H Me NC(O)C(O)H ¨CF3 H Me NC(O)C(O)Me ¨CF3 H Me NC(O)C(O)OMe ¨CF3 H Me NC(O)C(O)OEt ¨CF3 H Me NC(O)C(O)NH2CF3 H Me NC(O)C(O)OHCF3 H Me NC(NH)NH2 ¨CF3 H Me NC(NOH)NH2CF3 H Me NC(NH)NHMeCF3 H Me NC(NH)NMe2CF3 H Me NC(NH)OMeCF3 H Me NC(NH)OEtCF3 H Me NCOMe OCF3 H Me NCOEt OCF3 H Me NCOPr OCF3 H Me NCHO OCF3 H Me NCOiPr OCF3 H Me NCOtBu OCF3 H Me NCOPh OCF3 H Me NSO2Me OCF3 H Me NSO2Et OCF3 H Me NSO2Pr OCF3 H Me NSO2Ph OCF3 H Me NSO2iPr OCF3 H Me NNO2 OCF3 H Me NCOOMe OCF3 H Me NCOOEt OCF3 H Me NCOOPr OCF3 H Me NCOOiPr OCF3 H Me NCONHEt OCF3 H Me NCONHPr OCF3 H Me NCONH2 OCF3 H Me NCONHMe OCF3 H Me NCN OCF3 H Me NCOSMe OCF3 H Me NCOSEt OCF3 H Me NCSOMe OCF3 H Me NCSOEt OCF3 H Me NCSOPr OCF3 H Me NSO2NH2 OCF3 H Me NSO2NHMe OCF3 H Me NSO2NMe2 OCF3 H Me NP(O)(OMe)2 OCF3 H Me NP(O)(OEt)2 OCF3 H Me NP(O)Me2 OCF3 H Me NP(O)Et2 OCF3 H Me NP(O)Me(OMe) OCF3 H Me NP(O)(OPr)2 OCF3 H Me NC(O)C(O)H OCF3 H Me NC(O)C(O)Me OCF3 H Me NC(O)C(O)OMe OCF3 H Me NC(O)C(O)OEt OCF3 H Me NC(O)C(O)NH2 OCF3 H Me NC(O)C(O)OH OCF3 H Me NC(NH)NH2 OCF3 H Me NC(NOH)NH2 OCF3 H Me NC(NH)NHMe OCF3 H Me NC(NH)NMe2 OCF3 H Me NC(NH)OMe OCF3 H Me NC(NH)OEt OCF3 Me Me NCOMe ¨CF3 Me Me NCOEtCF3 Me Me NCOPrCF3 Me Me NCHOCF3 Me Me NCOiPrCF3 Me Me NCOtBuCF3 Me Me NCOPhCF3 Me Me NSO2MeCF3 Me Me NSO2Et ¨CF3 Me Me NSO2Pr ¨CF3 Me Me NSO2Ph ¨CF3 Me Me NSO2iPr ¨CF3 Me Me NNO2CF3 Me Me NCOOMeCF3 Me Me NCOOEt ¨CF3 Me Me NCOOPr ¨CF3 Me Me NCOOiPrCF3 Me Me NCONHEtCF3 Me Me NCONHPrCF3 Me Me NCONH2 ¨CF3 Me Me NCONHMe ¨CF3 Me Me NCN ¨CF3 Me Me NCOSMe ¨CF3 Me Me NCOSEt ¨CF3 Me Me NCSOMe ¨CF3 Me Me NCSOEt ¨CF3 Me Me NCSOPr ¨CF3 Me Me NSO2NH2 ¨CF3 Me Me NSO2NHMeCF3 Me Me NSO2NMe2CF3 Me Me NP(O)(OMe)2CF3 Me Me NP(O)(OEt)2CF3 Me Me NP(O)Me2CF3 Me Me NP(O)Et2CF3 Me Me NP(O)Me(OMe)CF3 Me Me NP(O)(OPr)2CF3 Me Me NC(O)C(O)HCF3 Me Me NC(O)C(O)Me ¨CF3 Me Me NC(O)C(O)OMe ¨CF3 Me Me NC(O)C(O)OEt ¨CF3 Me Me NC(O)C(O)NH2CF3 Me Me NC(O)C(O)OHCF3 Me Me NC(NH)NH2CF3 Me Me NC(NOH)NH2CF3 Me Me NC(NH)NHMeCF3 Me Me NC(NH)NMe2CF3 Me Me NC(NH)OMeCF3 Me Me NC(NH)OEt ¨CF3 Me Me NCOMe OCF3 Me Me NCOEt OCF3 Me Me NCOPr OCF3 Me Me NCHO OCF3 Me Me NCOiPr OCF3 Me Me NCOtBu OCF3 Me Me NCOPh OCF3 Me Me NSO2Me OCF3 Me Me NSO2Et OCF3 Me Me NSO2Pr OCF3 Me Me NSO2Ph OCF3 Me Me NSO2iPr OCF3 Me Me NNO2 OCF3 Me Me NCOOMe OCF3 Me Me NCOOEt OCF3 Me Me NCOOPr OCF3 Me Me NCOOiPr OCF3 Me Me NCONHEt OCF3 Me Me NCONHPr OCF3 Me Me NCONH2 OCF3 Me Me NCONHMe OCF3 Me Me NCN OCF3 Me Me NCOSMe OCF3 Me Me NCOSEt OCF3 Me Me NCSOMe OCF3 Me Me NCSOEt OCF3 Me Me NCSOPr OCF3 Me Me NSO2NH2 OCF3 Me Me NSONHMe OCF3 Me Me NSO2NMe2 OCF3 Me Me NP(O)(OMe)2 OCF3 Me Me NP(O)(OEt)2 OCF3 Me Me NP(O)Me2 OCF3 Me Me NP(O)Et2 OCF3 Me Me NP(O)Me(OMe) OCF3 Me Me NP(O)(OPr)2 OCF3 Me Me NC(O)C(O)H OCF3 Me Me NC(O)C(O)Me OCF3 Me Me NC(O)C(O)OMe OCF3 Me Me NC(O)C(O)OEt OCF3 Me Me NC(O)C(O)NH2 OCF3 Me Me NC(O)C(O)OH OCF3 Me Me NC(NH)NH2 OCF3 Me Me NC(NOH)NH2 OCF3 Me Me NC(NH)NHMe OCF3 Me Me NC(NH)NMe2 OCF3 Me Me NC(NH)OMe OCF3 Me Me NC(NH)OEt OCF3 Cl Cl NCOMeCF3 Cl Cl NCOEt ¨CF3 Cl Cl NCOPr ¨CF3 Cl Cl NCHO ¨CF3 Cl Cl NCOiPrCF3 Cl Cl NCOtBuCF3 Cl Cl NCOPh ¨CF3 Cl Cl NSO2Me ¨CF3 Cl Cl NSO2Et ¨CF3 Cl Cl NSO2Pr ¨CF3 Cl Cl NSO2Ph ¨CF3 Cl Cl NSO2iPr ¨CF3 Cl Cl NNO2 ¨CF3 Cl Cl NCOOMe ¨CF3 Cl Cl NCOOEt ¨CF3 Cl Cl NCOOPr ¨CF3 Cl Cl NCOOiPrCF3 Cl Cl NCONHEt ¨CF3 Cl Cl NCONHPr ¨CF3 Cl Cl NCONH2 ¨CF3 Cl Cl NCONHMe ¨CF3 Cl Cl NCN ¨CF3 Cl Cl NCOSMeCF3 Cl Cl NCOSEt ¨CF3 Cl Cl NCSOMe ¨CF3 Cl Cl NCSOEt ¨CF3 Cl Cl NCSOPr ¨CF3 Cl Cl NSO2NH2 ¨CF3 Cl Cl NSO2NHMe ¨CF3 Cl Cl NSO2NMe2 ¨CF3 Cl Cl NP(O)(OMe)2 ¨CF3 Cl Cl NP(O)(OEt)2CF3 Cl Cl NP(O)Me2 ¨CF3 Cl Cl NP(O)Et2CF3 Cl Cl NP(O)Me(OMe) ¨CF3 Cl Cl NP(O)(OPr)2 ¨CF3 Cl Cl NC(O)C(O)H ¨CF3 Cl Cl NC(O)C(O)Me ¨CF3 Cl Cl NC(O)C(O)OMe ¨CF3 Cl Cl NC(O)C(O)OEt ¨CF3 Cl Cl NC(O)C(O)NH2 ¨CF3 Cl Cl NC(O)C(O)OH ¨CF3 Cl Cl NC(NH)NH2 ¨CF3 Cl Cl NC(NOH)NH2CF3 Cl Cl NC(NH)NHMeCF3 Cl Cl NC(NH)NMe2CF3 Cl Cl NC(NH)OMe ¨CF3 Cl Cl NC(NH)OEtCF3 Cl Cl NCOMe OCF3 Cl Cl NCOEt OCF3 Cl Cl NCOPr OCF3 Cl Cl NCHO OCF3 Cl Cl NCOiPr OCF3 Cl Cl NCOtBu OCF3 Cl Cl NCOPh OCF3 Cl Cl NSO2Me OCF3 Cl Cl NSO2Et OCF3 Cl Cl NSO2Pr OCF3 Cl Cl NSO2Ph OCF3 Cl Cl NSO2iPr OCF3 Cl Cl NNO2 OCF3 Cl Cl NCOOMe OCF3 Cl Cl NCOOEt OCF3 Cl Cl NCOOPr OCF3 Cl Cl NCOOiPr OCF3 Cl Cl NCONHEt OCF3 Cl Cl NCONHPr OCF3 Cl Cl NCONH2 OCF3 Cl Cl NCONHMe OCF3 Cl Cl NCN OCF3 Cl Cl NCOSMe OCF3 Cl Cl NCOSEt OCF3 Cl Cl NCSOMe OCF3 Cl Cl NCSOEt OCF3 Cl Cl NCSOPr OCF3 Cl Cl NSO2NH2 OCF3 Cl Cl NSO2NHMe OCF3 Cl Cl NSO2NMe2 OCF3 Cl Cl NP(O)(OMe)2 OCF3 Cl Cl NP(O)(OEt)2 OCF3 Cl Cl NP(O)Me2 OCF3 Cl Cl NP(O)Et2 OCF3 Cl Cl NP(O)Me(OMe) OCF3 Cl Cl NP(O)(OPr)2 OCF3 Cl Cl NC(O)C(O)H OCF3 Cl Cl NC(O)C(O)Me OCF3 Cl Cl NC(O)C(O)OMe OCF3 Cl Cl NC(O)C(O)OEt OCF3 Cl Cl NC(O)C(O)NH2 OCF3 Cl Cl NC(O)C(O)OH OCF3 Cl Cl NC(NH)NH2 OCF3 Cl Cl NC(NOH)NH2 OCF3 Cl Cl NC(NH)NHMe OCF3 Cl Cl NC(NH)NMe2 OCF3 Cl Cl NC(NH)OMe OCF3 Cl Cl NC(NH)OEt OCF3 Cl H NCOMe ¨CF3 Cl H NCOEt ¨CF3 Cl H NCOPr ¨CF3 Cl H NCHOCF3 Cl H NCOiPr ¨CF3 Cl H NCOrBuCF3 Cl H NCOPh ¨CF3 Cl H NSO2Me ¨CF3 Cl H NSO2Et ¨CF3 Cl H NSO2PrCF3 Cl H NSO2Ph ¨CF3 Cl H NSO2iPr ¨CF3 Cl H NNO2 ¨CF3 Cl H NCOOMe ¨CF3 Cl H NCOOEt ¨CF3 Cl H NCOOPr ¨CF3 Cl H NCOOiPr ¨CF3 Cl H NCONHEt ¨CF3 Cl H NCONHPr ¨CF3 Cl H NCONH2CF3 Cl H NCONHMe ¨CF3 Cl H NCNCF3 Cl H NCOSMeCF3 Cl H NCOSEt ¨CF3 Cl H NCSOMe ¨CF3 Cl H NCSOEt ¨CF3 Cl H NCSOPr ¨CF3 Cl H NSO2NH2 ¨CF3 Cl H NSO2NHMe ¨CF3 Cl H NSO2NMe2 ¨CF3 Cl H NP(O)(OMe)2CF3 Cl H NP(O)(OEt)2 ¨CF3 Cl H NP(O)Me2CF3 Cl H NP(O)Et2CF3 Cl H NP(O)Me(OMe)CF3 Cl H NP(O)(OPr)2CF3 Cl H NC(O)C(O)HCF3 Cl H NC(O)C(O)MeCF3 Cl H NC(O)C(O)OMeCF3 Cl H NC(O)C(O)OEt ¨CF3 Cl H NC(O)C(O)NH2CF3 Cl H NC(O)C(O)OHCF3 Cl H NC(NH)NH2CF3 Cl H NC(NOH)NH2CF3 Cl H NC(NH)NHMeCF3 Cl H NC(NH)NMe2CF3 Cl H NC(NH)OMe ¨CF3 Cl H NC(NH)OEtCF3 Cl H NCOMe OCF3 Cl H NCOEt OCF3 Cl H NCOPr OCF3 Cl H NCHO OCF3 Cl H NCOiPr OCF3 Cl H NCOtBu OCF3 Cl H NCOPh OCF3 Cl H NSO2Me OCF3 Cl H NSO2Et OCF3 Cl H NSO2Pr OCF3 Cl H NSO2Ph OCF3 Cl H NSO2iPr OCF3 Cl H NNO2 OCF3 Cl H NCOOMe OCF3 Cl H NCOOEt OCF3 Cl H NCOOPr OCF3 Cl H NCOOiPr OCF3 Cl H NCONHEt OCF3 Cl H NCONHPr OCF3 Cl H NCONH2 OCF3 Cl H NCONHMe OCF3 Cl H NCN OCF3 Cl H NCOSMe OCF3 Cl H NCOSEt OCF3 Cl H NCSOMe OCF3 Cl H NCSOEt OCF3 Cl H NCSOPr OCF3 Cl H NSO2NH2 OCF3 Cl H NSO2NHMe OCF3 Cl H NSO2NMe2 OCF3 Cl H NP(O)(OMe)2 OCF3 Cl H NP(O)(OEt)2 OCF3 Cl H NP(O)Me2 OCF3 Cl H NP(O)Et2 OCF3 Cl H NP(O)Me(OMe) OCF3 Cl H NP(O)(OPr)2 OCF3 Cl H NC(O)C(O)H OCF3 Cl H NC(O)C(O)Me OCF3 Cl H NC(O)C(O)OMe OCF3 Cl H NC(O)C(O)OEt OCF3 Cl H NC(O)C(O)NH2 OCF3 Cl H NC(O)C(O)OH OCF3 Cl H NC(NH)NH2 OCF3 Cl H NC(NOH)NH2 OCF3 Cl H NC(NH)NHMe OCF3 Cl H NC(NH)NMe2 OCF3 Cl H NC(NH)OMe OCF3 Cl H NC(NH)OEt O表注: Et:乙基
Me:甲基
Pr:丙基
Ph:苯基
Bu:丁基
CN:氰基
组合物及应用方法
本发明提供杀虫组合物和使用在上面的本发明概述中给出的式(I)和式(II)化合物防治节肢动物、线虫、蠕虫和原虫害虫的方法。在优选的方面,本发明提供在一地点防治节肢动物或线虫的方法,所述的方法包含,将杀节肢动物或杀线虫有效量的式(I)或式(II)化合物或包含所述化合物和农业上可接受的载体的组合物,施用于所述的地点。在更优选的实施方案中,希望防治的节肢动物是昆虫,且在这一方面,本发明提供在一地点防治昆虫的方法,所述的方法包含,向所述的地点施用杀虫有效量的式(I)或式(II)化合物,或施用杀虫有效量的包含式(I)或式(II)化合物及其农业上可接受的载体的杀虫组合物。在另一优选的实施方案中,希望防治的节肢动物是线虫,且在这一方面,本发明提供在一地点防治线虫的方法,所述的方法包含,向所述的地点施用杀线虫有效量的式(I)或式(II)化合物,或施用杀线虫有效量的包含式(I)或(II)化合物及其农业上可接受的载体的杀线虫组合物。优选的是,施用杀节肢动物(特别是杀昆虫)或杀线虫有效量施用的地点是作物栽培区,即,作物生长或作物已经栽种的区域,或是作物将要种植/生长的区域。
本发明可用于杀虫,特别是杀节肢动物(特别是杀昆虫)或杀线虫、本发明处理的组合物,可以包含约0.001至约95%的式(I)或(II)活性成分。用于本文的“式(I)或(II)活性成分”或“活性成分”一词是指式(I)或(II)化合物或其盐。“式(I)或(II)化合物”的表达也在本文中使用,意指化合物或其盐。
施用于意欲处理的地点或作物的稀释液体制剂通常包含约0.001至约3%、优选约0.1至约0.5%的式(I)或(II)活性成分。
施用于所述地点或作物的固体制剂通常包含约?至约8%,优选约0.5至约5%的式(I)或式(II)活性成分。
浓缩的组合物是商业化的或运输或贮存的组合物。施用于植物时,它们通常用水稀释,且以这种稀释形式使用。稀释形式以及浓缩形式均是本发明的一部分。
浓缩的制剂通常包含约5至约95%,优选约10至约50%的式(I)或(II)活性成分。
本发明的杀虫组合物可以在整个昆虫生长季节一次或多次施用。本发明的杀虫组合物通常以约0.04至约2千克/公顷,优选约0.1至约1千克/公顷的活性成分的用量,施用于意欲处理的地点或作物区域。
本发明的浓缩杀虫组合物可以是固体(例如粉剂或颗粒剂或可湿性粉剂)的形式,或优选以液体(如乳油或真溶液)的形式。
本发明的组合物通常包含约0.5至约95%的活性成分。组合物的余量补齐至100%,包含载体以及如下文中提到的各种添加剂。
“载体”在本文中指的是有机或无机材料。所述的有机或无机材料可是天然或合成的,且可与活性成分一起且有利于活性成分施用于意欲处理的地点或作物。因此,此载体通常是惰性的且应当是农业上,特别是打算或处理的地点或作物可以接受的。载体可以是固体(陶土、硅酸盐、二氧化硅、树脂、蜡、肥料等)或液体(水、醇类、酮类、油溶剂、饱和或不饱和烃、氯代烃、液化石油气等)。
在众多的添加剂中,本发明的组合物可以包含表面活性剂以及其它成分如分散剂、粘着剂、消泡剂、抗冻剂、染料、增稠剂、粘合剂、保护性胶体、渗透剂、稳定剂、螯合剂、防絮凝剂、腐蚀抑制剂、颜料和聚合物。
更通常的是,本发明组合物可以包含所有各种固体或液体添加剂,它们是杀虫剂或杀虫处理领域已知的。
表面活性剂可以是乳化成润湿类型的离子或非离子表面活性剂。可能的表面活性剂是聚丙烯酸或木素磺酸的盐;苯酚磺酸或萘磺酸的盐;环氧乙烷与脂肪醇或脂肪酸或脂肪胺或取代的苯酚(特别是烷基苯酚或芳基苯酚)的缩聚物;磺基琥珀酸的酯盐;牛磺酸衍生物如烷基牛磺酸酯;磷酸酯;或醇或聚氧乙基化苯酚的酯。当喷雾载体是水时,通常需要使用至少一种表面活性剂,因为活性成分不是水溶性的。
本发明组合物的施用方法通常是将已经预先通过将更浓的本发明制剂制成的混合物稀释来喷雾。
固体组合物可以是用于撒粉或用于分散的粉剂(其中活性成分的含量可以多达100%)和颗粒剂,特别是挤出或压块型颗粒剂,或可以是已经通过掺合粉末制成的颗粒剂(在这种粉末中的活性成分的含量可以在约1至约80%之间)。
液体组合物或施用时须成为液体的组合物包括溶液、水溶性浓缩物、乳油、乳剂、可湿性粉剂或膏剂或可用水分散的颗粒剂。
乳油通常包含约10至约80%的活性成分;乳剂(当施用时)通常包含约0.01至约20%的活性成分。
例如,乳油可以包含溶剂和(至所需程度的)约2至约20%的适合的添加剂如稳定剂、表面活性剂、渗透剂、腐蚀抑制剂或其它已经提到的添加剂。
这些浓缩物通常于桶中水中稀释,以获得适合于喷雾的稀释液。
浓悬浮剂可以通过喷雾施用且须得是流动的,无任何固体分离和沉于底部。通常它们含有约1至约75%的活性成分(优选约2至约50%),约0.5至约15%的表面活性剂、约0.1至约10%的增稠剂和0至约10%的其它已经提到的适合的添加剂,余下的为水或有机液体(当活性成分是不溶或具有低溶解性时)。
可湿性粉剂通常包含活性成分(约1至约95%,优选约2至约80%)、固体载体、润湿剂(0至约5%)、分散剂(约3至约10%)和(至所需程度的)0至约10%的其它添加剂如稳定剂及已经列出的其它添加剂。
为了获得这些可湿性粉剂或喷粉剂,适合的是,将活性成分与添加剂混合如通过于磨或相似的设备中研磨。
可分散颗粒剂通常是通过将粉末附聚,接着通过适合的造粒工艺而制成。
本文中描述的乳剂可以是水包油或油包水型。乳剂的流动性可以是低粘性至接近凝胶粘性的高粘性。
在此诸多的组合物或制剂中,根据处理问题的具体条件,本领域技术人员可以选择出最适合的。
本发明的化合物或组合物也可以与其它农药例如杀虫剂、杀螨剂或除草剂混合。
本发明进一步通过下列实施例来说明,这些实施例不应被认为是限制本发明,给出之是为更好地应用本发明。
生物效力
下列代表性方法用来施用本发明化合物,并观察由之获得的生物活性:土壤浸渍蚜虫侵害的植物;对蝇施诱饵。
使用的种类如下:
属、种 俗名
Aphis gossypii 棉蚜
Schizaphis graminum 麦二叉蚜
Musca domestica 家蝇
土壤浸渍试验(内吸活性:蚜虫)
棉花和高粱植株长成于盆中。在处理前一天,各盆放上约25只混合虫口的蚜虫。以棉蚜侵染棉花而用麦二叉蚜侵染高梁。将选择的式(I)或(II)以稀释液施用于土壤表面,施用量相当于10.0ppm土壤浓度(按重量计)。蚜虫的计数在5DAT(即,处理后的天数)进行。将在处理植物上的蚜虫的数量与未处理对照植物上的蚜虫数比较。下列化合物显示出大于30%的棉蚜或是麦二叉蚜死亡率:1a、1b、3-29、30a、31-32。
家蝇诱饵/接触试验
将约25只四至六天大的家蝇成虫麻醉,并置于笼中,笼中放有含本发明化合物的糖水诱饵溶液。诱饵溶液中的本发明化合物浓度为100ppm。24小时后,刺激时,家蝇不动的被认为是死亡。下列化合物显示出大于30%的家蝇死亡率:1、1a、1b、2、3-10、12-14、16、18-20、22、25、26、28-30、30a、31、32。
虽然本发明已用各种优选的实施方案作为描述,但可以做出各种改进、替代、省略和改变而不偏离本发明的精神,这点对本发明技术人员而言是显而易见的。因此,本发明的范围旨在只受权利要求,包括其等同物范围的限制。