1616340-68-1Relevant articles and documents
Preparation method of multi-tenefavirin open-loop impurities and impurities thereof (by machine translation)
-
Paragraph 0071-0075, (2020/01/25)
Compared with the prior art, the method disclosed by the invention disclosed by the, invention is A simple in B reaction conditions, and the 1 reaction operation safety, of the 2 impurities of the 3, impurities of the impurities of the 4, impurities and the 5 impurities of the 6, A impurities 6 and the impurities of the impurities and the impurities of the A, impurities B; A B ; A B, A B, B. (by machine translation)
Method for synthesizing diastereomer impurity in dolutegravir raw material
-
Paragraph 0027-0030; 0031, (2019/11/13)
The invention provides a method for synthesizing a diastereomer impurity in a dolutegravir raw material, which comprises the following steps: 1, carrying out condensation reaction on SM1 serving as araw material and 2,4-difluorobenzylamine to generate a compound I; 2, reacting the compound I with an alkali in a reaction solvent to generate a compound II; 3, hydrolyzing the compound II under an acidic condition to generate a compound III; 4, carrying out acid catalytic reaction on the compound III and R-aminobutanol in a reaction solvent to generate a compound IV; 5, generating a compound V from the compound IV in a reaction solvent under the catalysis of a condensing agent; and 6, demethylating the compound V under the action of an alkali metal salt to generate an impurity VI. The synthetic method of the diastereoisomer impurity in the dolutegravir raw material is simple in process and available in raw material, and the prepared new impurity can provide a reference substance for quality analysis of dolutegravir, so that the quality standard of dolutegravir is improved.
A new method for preparing lu Tewei (by machine translation)
-
Paragraph 0029-0031; 0038-0040, (2017/08/28)
A process for preparing lu Tewei (E) new method, relates to the field of pharmaceutical chemistry, comprising the following steps: step 1) by the compound (A) with 2, 4 - two fluorine animal pen amine condensation reaction to obtain compound (B) steps 2) compound (B) removing the aldehyde protecting group to obtain the compound (C) step 3) compound (C) with R - 3 - amino - 1 - butanol on the ring by the reaction of the compound (D) step 4) compound (D) by the methylation reaction to occur after lu Tewei (E). This invention adopts the new line, and to the continuous optimization of the reaction conditions, so that the overall yield is raised greatly, as the compound (A) as a starting material and calculate the total yield is 75% or more, in a single reaction yield is 90% or more. (by machine translation)