摘要:
A process for preparing a 1-substituted 5-hydroxymethylimidazole of the formula: , wherein R represents alkyl, hydroxyalkyl, allyl, or substituted or unsubstituted arylmethyl or diarylmethyl, comprising the step of reacting a 1-substituted 2-mercapto-5-hydroxymethylimidazole of the formula: , wherein R is as defined above, in the presence of a transition metal catalyst and an oxidizing agent in a solvent.
摘要:
Starting from ethyl 3-(2,6-dichloro-5-fluoropyridin-3-yl)-3-oxo-propanoate (1), the present invention provides highly pure 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (5) in one-pot four steps using a single solvent.
摘要:
The present invention relates to a process for preparing 4-chloro-3-hydroxybutanoic acid ester, an intermediate for preparing atorvastatin, in high purity and yield, by comprising the steps of 1) reacting epichlorohydrin of formula (2) with cyanide of formula (3) under the condition of pH ranging from 7 to 8, to form the 4-chloro-3-hydroxybutyronitrile of formula (4) and 2a) dissolving the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent and reacting it with hydrogen chloride, or 2b) reacting the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent saturated with hydrogen chloride, to form the 4-chloro-3-hydroxybutyronitrile acid ester of formula (I).
摘要:
The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methane-sulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.
摘要翻译:本发明涉及制备喹诺酮抗生素关键中间体的4-氨基甲基-3-烷氧基亚氨基吡咯烷甲磺酸盐的方法。 根据本发明的方法,步骤总数已经缩短到2-3个步骤,不需要固体分离,并且使用昂贵的化学品,特别是(BOC)2 O (叔丁氧基羰基酐),几种有机溶剂和反应物。
摘要:
Starting from ethyl 3-(2,6-dichloro-5-fluoropyridin-3-yl)-3-oxo-propanoate (1), the present invention provides highly pure 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (5) inone-potfour stepsusing a single solvent.
摘要:
The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methanesulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.
摘要:
The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methanesulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.
摘要翻译:本发明涉及制备喹诺酮抗生素关键中间体的4-氨基甲基-3-烷氧基亚氨基吡咯烷甲磺酸盐的方法。 根据本发明的方法,步骤总数已经缩短到2-3个步骤,不需要固体分离,并且使用昂贵的化学品,特别是(BOC)2 O (叔丁氧基羰基酐),几种有机溶剂和反应物。
摘要:
The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methane-sulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.
摘要翻译:本发明涉及制备喹诺酮抗生素关键中间体的4-氨基甲基-3-烷氧基亚氨基吡咯烷甲磺酸盐的方法。 根据本发明的方法,步骤总数已经缩短到2-3个步骤,不需要固体分离,并且使用昂贵的化学品,特别是(BOC)2 O (叔丁氧基羰基酐),几种有机溶剂和反应物。