Patent ID: 6924377

Claim:
A process for preparing a compound of formula I wherein: R 1 is H, (C 1 -C 8 )alkyl, (C 3 -C 7 )cycloalkyl, aryl, (CH 2 ) n -aryl, heterocyclo, (CH 2 ) n -heterocyclo, heteroaryl, or (CH 2 ) n -heteroaryl, wherein n is 0, 1, 2, or 3; and R 2 and R 2′ , are each independently H, straight or branched (C 1 -C 6 )alkyl, a straight or branched (C 2 -C 7 )alkenyl, (C 3 -C 7 )cycloalkyl, alkylcycloalkyl, alkylalkoxy, alkylphenyl, alkyphenoxy, phenyl or substituted phenyl; comprising: (a) treating mucochloric or mucobromic acid 1 wherein X is Cl or Br with R′OH, wherein R′ is (C 1 -C 6 )alkyl, −CH 2 -phenyl, or —CH 2 -substituted phenyl in the presence of acid to provide 2A (b) conjugate addition of R 2 R 2′ CHM 0 wherein R 2 and R 2′ are as defined above and wherein M 0 is MgBr, CuBr, or B(OH) 2 , to 2A, to provide 3A (c) hydrogenation of 3A to provide 4A (d) reductive amination of 4A under hydrogenation conditions using ammonium formate or R 1a NH 2 , wherein R 1a is H, (C 1 -C 8 )alkyl, (C 3 -C 7 )cycloalkyl, aryl, (CH 2 ) n -aryl, (CH 2 ) n —CH—[(C 1 -C 3 )alkyl](aryl), heterocyclo, (CH 2 ) n -heterocyclo, heteroaryl, or (CH 2 ) n -heteroaryl, wherein n is 0, 1, 2, or 3 and p is 0, 1, 2, or 2, followed by hydrolysis