abstract |
1455998 2 - [α - (Substituted) - aminobenzyl] - 1,3 - propanediols ELI LILLY & CO 10 Dec 1973 [8 Dec 1972] 29003/76 Divided out of 1455997 Heading C2C Novel compounds of Formula I wherein R and R<SP>1</SP> are C 1 -C 4 alkyl or C 2 -C 4 alkenyl or when taken together with the nitrogen to which they are attached, are aziridino, pyrrolidino or piperidino; and Ar is phenyl, halophenyl, methoxyphenyl, methylphenyl, trifluoromethylphenyl, hydroxyphenyl, acetoxyphenyl, benzyloxyphenyl, or 3-pyridyl as well as compounds wherein R<SP>1</SP> is also H or benzyl and R is also benzyl are prepared by reacting a di-C 1-6 -alkylbenzalmalonate with an amine of formula HNRR<SP>1</SP> to form an intermediate di- C 1-6 -alkyl-(α-RR<SP>1</SP>N-)-benzylmalonate which is reduced to give a comound of Formula I. The dialkyl benzal malonate is obtained by reacting a substituted benzaldehyde ArCHO with a dialkyl malonate. |