BLEND Duglas K. (US),БЛЭНД Дуглас К. (US),ROSS Ronald Ml. (US),РОСС Рональд Мл. (US),DZHONSON Piter L. (US),ДЖОНСОН Питер Л. (US),DZHONSON Timoti S. (US),ДЖОНСОН Тимоти С. (US),BLEND Duglas K.,БЛЭНД Дуглас К.,ROSS Ronald Ml.,РОСС Рональд Мл.,DZHONSON Piter L.,ДЖОНСОН Питер Л.,DZHONSON Timoti S.,ДЖОНСОН Тимоти С.
申请号：
RU2015102948
公开号：
RU0002628339C2
申请日:
2013.06.12
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: for the preparation of the 2-substituted-5-(1-alkylthio)-alkyl-pyridine-N-oxide corresponding to formula (I):where L is a single bond or R1, S and L taken together are 4-, 5- or 6-membered ring； R1 is (C1-C4) -alkyl； R2 and R3 are individually hydrogen, methyl, ethyl, fluoro, chloro or bromo； N is an integer from 0 to 3； And Y is (C1-C4)-haloalkyl； In which: (i) the enamine corresponding to formula (II):,where R1, R2, R3, L and n are as defined above； And R4 and R5 are independently C1-C8-alkyl, C2-C8-alkenyl, C1-C8-arylalkyl, C1-C8-haloalkyl, C1-C8-alkoxyalkyl, C1-C8-alkylaminoalkyl, aryl or heteroaryl, or R4 and R5, taken together with N, represent a 5- or 6-membered saturated or unsaturated ring； is condensed with an α, α-unsaturated ketone corresponding to formula (III):,where Y is as defined above； and X1 is halogen, OR6, OSO2R6, SR6, SOR6, SO2R6 or NR7R8, where R6 is hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C8-arylalkyl, C1-C8-haloalkyl, C1-C8-alkoxyalkyl, C1-C8-alkylaminoalkyl, aryl or heteroaryl, and R7 and R8 are independently hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C8-arylalkyl, C1-C8-haloalkyl, C1-C8-alkoxyalkyl, C1-C8-alkylaminoalkyl, aryl or heteroaryl, or R7 and R8 taken together with N are a 5- or 6-membered saturated or unsaturated ring； to obtain an intermediate corresponding to formula (IV):,where R1, R2, R3, R4, R5, L and n are as defined above； and (ii) the intermediate corresponding to formula (IV) is cyclized using an amine nucleophile corresponding to formula (V): H2N-X2, wherein X2 is hydroxyl, alkoxy, cyano, amino or mercaptan.EFFECT: invention enables realisation of the mentioned purpose.21 cl, 2 tbl, 7 exИзобретение относится к сельскому хозяйству. Для получения 2-замещенного-5-(1-алкилтио)алкил-пиридин-N-оксида, соответствующего формуле (I):,где L представляет собой одинарную связь или R1, S и L, взятые вместе, представляют собой 4-, 5- или 6-членное кольцо； R1 представляет собой (С1-С4)-алкил； R2 и R3 по отде
