Preparation of alethine derivative

Abstract

Abstract PURPOSE: To prepare an N-substituted alethine in high yield and purity, by reacting an N-substituted-β-alanine with cystamine or cysteamine in the presence of a deacidifying agent, a halogen compound, a tertiary phosphine or a tertiary phosphite. CONSTITUTION: An N-substituted alethine is prepared by the direct condensation of an N-substituted-β-alanine with cystamine or cysteamine, or their salts, in the presence of a halogen compound such as halogen molecule, alkyl halide, etc., a tertiary phosphine such as triphenyl phosphine, or a tertiary phosphite. The N- substitution group is an amino-protecting group such as acyl group. The reaction is pref. carried out in an organic base as a solvent to remove the by-produced hydrogen halide from the system. EFFECT: The objective compound can be obtained economically, by a simple process. USE: Pharmacenticals or their intermediates. COPYRIGHT: (C)1980,JPO&Japio

Inventors

• 👤 Masahiro Kamata
• 👤 Akihiko Miyadera

Bibliographic Details