首页> 外国专利> Process for the preparation of a compound compound r, s- (z) -alpha- (oximino-alpha- (1-azabicyclo) 2.2.2 -oct-3-yl) acetonitrile zwitterionic r- (z) - alpha- (oximino) -alpha- (1-azabicyclo) 2.2.2 -oct-3-yl) acetonitrile zwitterionic acid alpha -cyano-1-azabicyclo 2.2.2 -octane-3-acetic process for resolving r, s -alpha- (methoximino) -alpha- (1-azabicyclo) 2.2.2 -oct-3-yl) acetonitrile and process for the solution of r, s- (z) - alpha (oximino) - alpha (1-azabicycles 2.2.2 -oct-3-yl) acetonitrile and process for the preparation of r- (z) - alpha- (methoxyimino) -alpha- (1-azabicycles) 2.2.2 -oct-3-yl) acetonitrile

Process for the preparation of a compound compound r, s- (z) -alpha- (oximino-alpha- (1-azabicyclo) 2.2.2 -oct-3-yl) acetonitrile zwitterionic r- (z) - alpha- (oximino) -alpha- (1-azabicyclo) 2.2.2 -oct-3-yl) acetonitrile zwitterionic acid alpha -cyano-1-azabicyclo 2.2.2 -octane-3-acetic process for resolving r, s -alpha- (methoximino) -alpha- (1-azabicyclo) 2.2.2 -oct-3-yl) acetonitrile and process for the solution of r, s- (z) - alpha (oximino) - alpha (1-azabicycles 2.2.2 -oct-3-yl) acetonitrile and process for the preparation of r- (z) - alpha- (methoxyimino) -alpha- (1-azabicycles) 2.2.2 -oct-3-yl) acetonitrile

机译:制备化合物[r,s-(z)-α-(肟基-α-(1-氮杂双环)[2.2.2] -oct-3-yl)乙腈两性离子[r-(z)-的方法α-(肟基)-α-(1-氮杂双环)[2.2.2]-辛-3-基)乙腈两性离子酸α-氰基-1-氮杂双环[2.2.2]-辛烷-3-乙酸法[ r,s] -alpha-(甲氧亚氨基)-alpha-(1-氮杂双环)[2.2.2] -oct-3-yl)乙腈和[r,s-(z)]-α(oximino的溶液的制备方法)-α(1-氮杂双环[2.2.2]-辛-3-基)乙腈和制备[r-(z)]-α-(甲氧基亚氨基)-α-(1-氮杂双环)的方法[2.2。 2] -oct-3-yl)乙腈

摘要

A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: IMAGE (I) wherein R1 represents IMAGE in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1; R2 is a group OR4, where R4 is C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl or a group OCOR5 where R5 is hydrogen or R4; and R3 is CN; said process comprising reacting a compound of formula (II): IMAGE (II) wherein R1' is R1 or a group convertible thereto, and R3' is an electron withdrawing group, with a source of nitrous acid, and thereafter converting the resulting =NOH group to =NR2 wherein R2 is as defined in formula (I), converting R1' and R3' when other than R1 and R3 to R1 and R3, and thereafter optionally forming a pharmaceutically acceptable salt.
机译:式(I)化合物或其药学上可接受的盐的制备方法:(I)其中R1代表,其中r代表2至4的整数,s代表1或2,t代表0或1; R 2为基团OR 4,其中R 4为C 1-4烷基,C 2-4烯基或C 2-4炔基或基团OCOR 5,其中R 5为氢或R 4; R3为CN;所述方法包括使式(II)的化合物与亚硝酸源反应:其中R 1'为R 1或可转化为基团,且R 3'为吸电子基团的式(II)与亚硝酸源反应,然后转化所得= NOH基团== NR2基团,其中R2如式(I)中所定义,将R1和R3以外的R1′和R3′转化为R1和R3,然后任选地形成药学上可接受的盐。

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