88069-56-1Relevant articles and documents
Preparation method of intermediate of synthesis of pilsicainide hydrochloride
-
Paragraph 0078-0087, (2019/07/11)
The invention provides a preparation method of an intermediate for synthesis of pilsicainide hydrochloride. The method comprises the following steps: step 1, performing a polymerization reaction on butyrolactam (I) and gamma-butyrolactone (II) under strong base and predetermined conditions to form N-(3-carboxypropyl)butyrolactam (III); step 2, performing cyclization on the N-(3-carboxypropyl)butyrolactam(III) at a high temperature in a monoisopropyl malonate solvent, performing condensation on the cyclization product and a monoester malonate to form 7alpha-pyrrolizine-acetate, wherein preferred choice is to produce 7alpha-pyrrolizine-isopropyl acetate (V); and step 3, performing hydrolysis on the 7alpha-pyrrolizine-acetate in an acid to form the corresponding pharmaceutically-acceptable salt. The preparation method provided by the invention avoids expensive or difficult-to-obtain raw materials, avoids use of liquid ammonia in the synthetic process, reduces the reaction steps, and has simple operation, less three waste (waste water, waste gas and solid waste) and a high yield.
The novel preparation methods of 5-substituted methyl-1 -azabicyclo[3.3.0]octane
Oka, Mitsuru,Baba, Kunihisa,Suzuki, Tomoo,Matsumoto, Yukiharu
, p. 2317 - 2320 (2007/10/03)
5-Substituted methyl-1-azabicyclo[3.3.0]octane, which is a useful intermediate for drugs, was readily synthesized from 1,7-dichloro-4-heptanone without isolating unstable intermediates.
