Methylaminoacetonitrile hydrochloride

Yellow crystal

Methylaminoacetonitrile hydrochloride can be used as an intermediate in pharmaceutical and chemical synthesis. It is the raw material for the preparation of tadalafil. Approved by the FDA in 2003, tadalafil was marketed in the United States as a drug for the treatment of erectile dysfunction in men.

A method of preparing methylaminoacetonitrile hydrochloride, comprising: (1) reacting methylamine hydrochloride, sodium cyanide and formaldehyde as reaction raw materials to form methylaminoacetonitrile in the presence of a catalyst; and (2) reacting said methylaminoacetonitrile with hydrochloric acid to form said methylaminoacetonitrile hydrochloride, and in step (1) the reaction is carried out at below 0 C. using 3-mercaptopropionic acid as a catalyst, and the amount of catalyst is from 0.9 to 1.1 times.