61381-04-2Relevant articles and documents
Novel method for preparing drotaverine hydrochloride intermediate
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, (2020/06/16)
The invention discloses a novel method for preparing a drotaverine hydrochloride intermediate, belonging to the technical field of medicine synthesis. The preparation method comprises the following steps: preparing an intermediate 3,4-diethoxyphenylacetic acid with 1,2-diethoxybenzene as a raw material, and preparing the intermediate 3,4-diethoxyphenylacetamide with 3,4-diethoxyphenylacetic acid as a raw material. According to the novel process for preparing the drotaverine hydrochloride intermediate, a method for directly preparing 3,4-diethoxyphenylacetic acid and 3,4-diethoxyphenylethylamine is adopted, and a process for preparing 3,4-diethoxyphenylacetonitrile is avoided, so a reaction step of using sodium cyanide is avoided.
Novel preparation method of drotaverine hydrochloride intermediate
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, (2019/06/27)
The invention discloses a novel preparation method of a drotaverine hydrochloride intermediate. The preparation method comprises the steps that 1, 4-bromopyrocatechol serves as the raw material and issubjected to an ethylation reaction under the action of iodoethane or diethyl sulfate, and 1,2-diethoxy-4-bromobenzene is prepared; 2, 1,2-diethoxy-4-bromobenzene is subjected to a Suzuki-Miyaura coupling reaction and reacts with ethyl bromoacetate or methyl bromoacetate to prepare 3,4-diethoxyphenylaceticacid ester; 3, 3,4-diethoxyphenylaceticacid is hydrolyzed to prepare 3,4-diethoxyphenylaceticacid; 4, 3,4-diethoxyphenylaceticacid ester and ammonia are prepared into 3,4-diethoxyphenylacetamide; 5, 3,4-diethoxyphenylacetamide is reduced to prepare 3,4-diethoxyphenethylamine. The direct preparation method is used; in the process of preparing 3,4-diethoxyphenyl acetonitrile, application of sodium cyanide is avoided; when 3,4-diethoxyphenethylamine is prepared, lithium aluminium hydride isused for reduction, and a pressurized hydrogenation method is prevented from being used, so that the problems about safety and environment pollution are effectively solved, the process is simple andeasy to implement, and the practicality is high.
Novel dihydroquinolizinones for the treatment and prophylaxis of hepatitis B virus infection
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Paragraph 1090; 1091, (2015/08/04)
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and R6 are as described herein, compositions including the compounds and methods of using the compounds.
NOVEL DIHYDROQUINOLIZINONES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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Page/Page column 132, (2015/09/23)
The invention provides novel compounds having the general formula (I) wherein R1, R2 R3, R4, R5 and R6 are as described herein, compositions including the compounds and methods of using the compounds in the treatment of the hepatitis B virus.
BRIDGED SIX-MEMBERED RING COMPOUNDS
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Page/Page column 84, (2008/12/08)
The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
Process for the preparation of (8As,12AS,13AS)-decahydroisoquino ((2,1-G) (1,6)-naphthyridin-8-one derivatives
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, (2008/06/13)
The invention provides a process for preparing single enantiomers of compounds represented by the formula: STR1 and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy; which includes reduction of a compound represented by the formula: STR2 to give a mixture of stereoisomers represented by the formula: STR3 wherein each wavy line independently represents a bond in either the α or β position; followed by dissolving the mixture of stereoisomers and a chiral resolving acid in a suitable solvent and allowing the solution to crystallize, giving a salt of the desired enantiomer.