- NOVEL PROCESS FOR THE PREPARATION OF LERCANIDIPINE
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The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of
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Page/Page column 3
(2009/09/26)
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- PROCESS FOR PREPARING LERCANIDIPINE HYDROCHLORIDE
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Disclosed herein is a novel method for preparing lercanidipine hydrochloride which is highly effective for treating hypertension. The method comprises the steps of reacting 2,6-dimethyl-5-methoxycarbonyl-4-(3- nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid with a substituted chlorophosphate derivative to obtain a substituted phosphonoester derivative, and reacting the substituted phosphonoester derivative with 2, N-dimethyl-N- (3,3-diphenylpropyl)-1-amino-2-propanol. According to the preparation method, since little by-products are formed, the yield is improved, as compared to cases of conventional methods. In addition, the method involves simple isolation and purification processes of lercanidipine, thus realizing a high-quality product. Furthermore, the method has advantages of low preparation costs, substantial waste-free environmental-friendly process and applicability to industrial mass-production.
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Page/Page column 7-8
(2008/12/07)
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- LERCANIDIPINE HYDROCHLORIDE POLYMORPHS AND AN IMPROVED PROCESS FOR PREPARATION OF 1,1,N-TRIMETHYL-N-(3,3-DIPHENYLPROPYL)-2-AMINOETHYL ACETOACETATE
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Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of substantially pure Lercanidipine intermediate, 1,1,N- trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl acetoacetate. The intermediate is useful for preparing Lercanidipine, or a pharmaceutically acceptable salt thereof, in high yield and purity. The present invention further provides a novel crystalline form of Lercanidipine hydrochloride and a process for its preparation. The present invention also provides a process for the preparation of amorphous form of Lercanidipine hydrochloride.
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- PROCESS FOR PREPARING AMORPHOUS LERCANIDIPINE HYDROCHLORIDE
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The invention provides a process for preparing substantially pure amorphous lercanidipine hydrochloride. The amorphous lercanidipine hydrochloride prepared as disclosed herein is substantially pure and has a greater aqueous solubility and faster onset of
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Page/Page column 7
(2008/06/13)
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- Process for Producing Lercanidipine
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A process for preparing 1,4-dihydro-2,6-dimethyl-4- (3-nitrophenyl) -3,5-pyridinedicarboxylic acid 2- [(3,3-diphenyl-propyl) methylamino]-1,1-dimethylethyl ester (Lercanidipine) I, which comprises reacting 1,4-dihydro-2,6-dimethyl-4- (3-nitrophenyl) -3,5-
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Page/Page column 1; 8; 15
(2010/11/29)
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- POLYMORPHIC FORM OF LERCANIDIPINE HYDROCHLORIDE AND PROCESS FOR THE PREPARATION THEREOF
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Processes for the purification of lercanidipine hydrochloride are provided which uses a binary system of an alcohol-containing solvent such as methanol and an aliphatic ester-containing solvent such as isopropyl acetate. Processes for the preparation of s
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Page/Page column 22-23
(2008/06/13)
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- INTERMEDIATES FOR THE PREPARATION OF LERCANIDIPINE
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Intermediates for the preparation of Lercanidipine comprising 1-halo-2-methyl-2-propyl methyl-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-1-pyridine-3,5-dicarboxylate of the formula.
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