Patent ID: 6060607
Filing Date: 2000-05-09
Classification: C07D,C07F

Abstract:
A process of producing a compound of the formula 5: ##STR72## wherein P is diisopropylphosphoryl; R.sup.1 and R.sup.2 are independently selected from hydrogen, aryl and heteroaryl, said aryl and heteroaryl groups being unsubstituted or substituted with from 1-3 groups selected from the group consisting of: C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo, hydroxy, CO.sub.2 H, CO.sub.2 C.sub.1-4 alkyl, NH.sub.2, NHC.sub.1-4 alkyl, N(C.sub.1-4 alkyl).sub.2, SO.sub.3 H, CN, NHC(O)C.sub.1-4 alkyl, SO.sub.2 NH.sub.2, SO.sub.2 C.sub.1-4 alkyl, aryl and heteroaryl;comprising: (a) reacting a compound of the formula 2: ##STR73## wherein P is as previously defined with diphenylphosphinic chloride to produce a compound of the formula 3: ##STR74## (b) reacting compound 3 with methanesulfonyl chloride to produce a compound of formula 4: ##STR75## (c) combining compound 4 with an alkali metal sulfide or non-alkali metal sulfide in water to produce a compound of formula 1: ##STR76## and (d) reacting compound 1 with NHR.sup.1 R.sup.2 in the presence of an organic acid wherein R.sup.1 and R.sup.2 are as previously defined to produce a compound of formula 5.