PROCESS FOR THE PREPARATION OF DIHYDROPYRROLE DERIVATIVES

摘要

The present invention provides stereoselective processes for the preparation of compounds of formula (I);whereinP is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted;R1 is chlorodifluoromethyl or trifluoromethyl;R2 is optionally substituted aryl or optionally substituted heteroaryl;n is 0 or 1;including the process comprising(a-i) reacting a compound of formula II;wherein P, R1 and R2 are as defined for the compound of formula I;with nitromethane in the presence a chiral catalyst to give a compound of formula III;wherein P, R1 and R2 are as defined for the compound of formula I; and(a-ii) reductively cyclising the compound of formula III to give the compound of formula I.;The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).

主权项

1. A compound of formula I, or a salt of N-oxide thereof,or
a compound of formula III, or a salt of N-oxide thereof,or
a compound of formula IV, or a salt of N-oxide thereof,or
a compound of formula XXIII, or a salt of N-oxide thereof, a compound of formula XXIV, or a salt of N-oxide thereof, wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; n is 0 or 1; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is optionally substituted aryl or optionally substituted heteroaryl; W is hydrogen or optionally substituted aryl; Y is optionally substituted aryl; and Z is optionally substituted alkyl or optionally substituted arylalkylene.