- Novel process for preparing 1-methyl-2-(2-hydroxyethyl)pyrrolidine
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The present invention relates to a method for synthesizing 1-methyl-2-(2-hydroxyethyl)pyrrolidine, which is useful as an intermediate of a pharmaceutical. More specifically, the present invention relates to a novel synthesis method which uses metal borohydride as a reducing agent in a process of manufacturing 1-methyl-2-(2-hydroxyethyl)pyrrolidine, which is a target substance, from methyl (2E/Z)-2-(1-methylpyrrolidinyridin-2-ylidene)acetate, wherein the methyl (2E/Z)-2-(1-methylpyrrolidinyridin-2-ylidene)acetate is reduced in two stages sequentially, thereby being able to obtain the target substance with a safe process and cheap cost compared to an existing method.COPYRIGHT KIPO 2020
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- An efficient process of preparation of 1-methyl-2-(2-hydroxyethyl)pyrrolidine for production in ton scale
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The present invention relates to a safe, simple and novel manufacturing method of 1-methyl-2-(2-hydroxyethyl)pyrrolidine as a drug medium, capable of mass production. 1-methyl-2-(2-hydroxyethyl)pyrrolidine can be manufactured by: reducing a double bond into a single bond through hydrogenation reaction in the presence of palladium on carbon (Pd on C) catalyst, and sequentially reducing an ester group into an alcohol group with a reducing agent such as NaBH_4 or LiBH_4; reducing a double bond and an ester group at a single reaction at the same time; or performing enantioselective hydrogenation of allylic alcohol with a chiral catalyst.
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- Biomimetic oxidation of clemastine fumarate
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The reaction of clemastine fumarate (1) with the biomimetic system manganese(III)-5,10,15,20-tetrakis(pentafluorophenyl)porphyrin chloride (MnTPFPPCl)/imidazole/hydrogen peroxide in a mixture of dichlormethane/methanol affords several metabolites. These compounds are products of O-dealkylation, N-demethylation, N-oxidation and separation of water. The reaction of 1 in aqueous solution with manganese(III)-5,10,15,20-tetrakis(pentafluorophenyl)-β-tetrasulfonat oporphyrin chloride (MnTPFPS4PCl) as catalyst additional generates products of aromatic hydroxylation. Products were identified by TLC, UV, and MS. Thereby we found a close conformity with rat metabolism.
- Froehlich,Pietzyk,Smolinka,Goeber
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p. 409 - 414
(2007/10/03)
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