88069-56-1Relevant articles and documents
Preparation method of intermediate of synthesis of pilsicainide hydrochloride
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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.
Facile entry to ethyl tetrahydro-1H-pyrrolizin-7a(5H)-ylacetate: A versatile pharmaceutical intermediate
Bruno, Claudio,Catalano, Alessia,Lentini, Giovanni,Carocci, Alessia,Franchini, Carlo,Tortorella, Vincenzo
experimental part, p. 2193 - 2200 (2011/04/17)
An improved synthesis of ethyl tetrahydro-1H-pyrrolizin-7a(5H)-ylacetate is reported. This valuable pharmaceutical intermediate was easily obtained from 1,7-diiodo-4-heptanone in 46% yield, thus improving the procedure reported in the literature (23% yield) which starts from 1,7-dichloro-4-heptanone. Moreover, 1,7-diiodo-4-heptanone was obtained as an easily manageable solid, in this being preferable to its 1,7-dichloro isologue, which is a quite unstable oil. The former was synthesized in high overall yield (75%) starting from the commercially available diethyl 4-oxoheptanedioate, thus overtaking the well-known problems related to the use of γ-butyrolactone. The Japan Institute of Heterocyclic Chemistry.
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.
New Anthiarrythmic Agents. N-Aryl-8-pyrrolizidinealkanamides
Miyano, Seiji,Sumoto, Kunihiro,Satoh, Fumio,Shima, Keiyu,Hayashimatsu, Mariko,et al.
, p. 714 - 717 (2007/10/02)
The synthesis and antiarrhytmic activity of N-aryl-8-pyrrolizidinealkanamides are described.The targed compounds were evaluated for their ability to protect against chloroform-induced fibrillation in mice.Many of them were found to have antifibrillatory activity comparable to that of lidocaine; several are more potent than lidocaine.N-(2,6-Dimethylphenyl)-8-pyrrolizidineacetamide (6n), which was found to be more potent and less toxic (LD50) than lidocaine, also showed a long duration of action in dogs with venticular arrhythmias after oral administration.
