154212-60-9Relevant articles and documents
A N - methyl -2 - isopropyl -4 - thiazole preparation of method
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Paragraph 0016; 0018; 0019; 0021, (2019/04/06)
The present invention provides a N - methyl - 2 - isopropyl - 4 - thiazole preparation of method, relates to the technical field of drug synthesis, solves the problem of the ritonavir intermediate N - methyl - 2 - isopropyl - 4 - thiazole preparation of method the existence of toxicity is relatively large, not friendly to the environment the technical problem. The preparation method comprises the following steps: (1) acylated - cyclization reaction; (2) aromatization - substitution reaction; (3) reduction reaction. The invention provides N - methyl - 2 - isopropyl - 4 - thiazole preparation of method, through to the cheap and easy isobutyryl chloride with cysteine methyl ester hydrochloride as raw materials; - cyclization reaction by acylation, aromatization - substitution reaction, the reduction reaction of the three-step synthesizing the compound; compared with the prior preparation method, has environmental protection of green, easy large-scale industrial production and yield and the like, has good application prospect.
Preparation method for 2-isopropyl-4-(methyl aminomethyl) thiazole hydrochloride
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Paragraph 0042-0044, (2018/04/01)
The invention belongs to the field of medical intermediate synthesis, relates to a preparation method for ritonavir intermediate synthesis and particularly relates to a preparation method for 2-isopropyl-4-(methyl aminomethyl) thiazole hydrochloride. Isobutyric acid firstly reacts with thionyl chloride, and then ammonium sulfide and ammonium hydroxide are subjected to sulfo-reaction and aminating reaction, the existing process of using phosphorus pentasulfide for performing sulfo-reaction after acylation is replaced, the heavy smell is prevented from generating in the preparation process to avoid the environmental pollution. According to the invention, 1,3-dihydroxy acetone is adopted for replacing 1,3-dichloroacetone with high price, heavy smell and high pollution, the cost is saved and the preparation is environmentally friendly. According to the preparation method provided by the invention, the process is simple, the yield higher than that of the prior art and the preparation method is suitable for industrial production.
ACID ADDITION SALT OF 2-ISOPROPYL-4-(((N-METHYL)AMINO)METHYL)THIAZOLE AND ITS?USE IN THE PREPARATION OF RITONAVIR
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Page/Page column 8-9, (2008/06/13)
The present invention relates to a novel acid addition salt of 2-Isopropyl-4-(((N-methyl)amino)methyl)thiazole of Formula (I) which is a useful intermediate for preparing HIV protease inhibitors. The present invention further provides a process for preparing ritonavir, a HIV protease inhibitor, using the compound of Formula (I).