Process for producing 2-amino-2- [2- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] ethyl] -1,3-propanediol hydrochloride and hydrates thereof, and intermediates for the production thereof
A process for producing 2-amino-2- [2- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] ethyl] -1,3-propanediol hydrochloride or a hydrate thereof, comprising the steps of: reacting 4- (3-benzyloxyphenylthio) -2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to form ethyl 3- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] acrylate； reduce the resulting ethyl 3- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] acrylate, followed by mesylation, iodination and nitration, to form 1-benzyloxy-3- [3-chloro-4- (3- nitropropyl) phenylthio] benzene； hydroxymethylate the resulting 1-benzyloxy-3- [3-chloro-4- (3-nitropropyl) phenylthio] benzene with formaldehyde to form 2- [2- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] ethyl] - 2-nitro-1,3-propanediol； and reduce the resulting 2- [2- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] ethyl] -2-nitro-1,3-propanediol to form the desired product.Un procedimiento para producir hidrocloruro de 2-amino-2-[2-[4-(3-benciloxifeniltio)-2-clorofenil]etil]-1,3- propanodiol o un hidrato del mismo, que comprende las etapas de: hacer reaccionar el 4-(3-benciloxifeniltio)-2-clorobenzaldehído con dietilfosfonoacetato de etilo en un disolvente en presencia de una base para formar el 3-[4-(3-benciloxifeniltio)-2-clorofenil]acrilato de etilo； reducir el 3-[4-(3-benciloxifeniltio)-2-clorofenil]acrilato de etilo resultante, seguido de la mesilación, yodación y nitración, para formar el 1-benciloxi-3-[3-cloro-4-(3-nitropropil)feniltio]benceno； hidroximetilar el 1-benciloxi-3-[3-cloro-4-(3-nitropropil)feniltio]benceno resultante con formaldehído para formar el 2-[2-[4-(3-benciloxifeniltio)-2-clorofenil]etil]-2-nitro-1,3-propanodiol； y reducir el 2-[2-[4-(3-benciloxifeniltio)-2-clorofenil]etil]-2-nitro-1,3-propanodiol resultante para formar el producto deseado.
