- METHOD OF PREPARING(3R,5R)-7-(2-(4-FLUOROPHENYL)-5-ISOPROPYL-3-PHENYL-4-((4-HYDROXYMETHYLPHENYLAMINO)CARBONYL)-PYRROL-1-YL)-3,5-DIHYDROXY-HEPTANOIC ACID HEMI CALCIUM SALT, AND METHOD OF PREPARING INTERMEDIATES USED THEREIN
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The present invention provides a method for preparing (3R,5R)-7-(2-(4-flurophenyl)-5-isopropyl-3-phenyl-4-((4-hydroxymethylphenylamino)carbonyl)-pyrrole-1-yl)-3,5-dihydroxy heptanoic acid hemicalcium salt. The preparation method of the present invention is performed in a convergent synthesis manner in which main structural moieties of a (3R,5R)-7-(2-(4-flurophenyl)-5-isopropyl-3-phenyl-4-((4-hydroxymethylphenylamino)carbonyl)-pyrrole-1-yl)-3,5-dihydroxy heptanoic acid hemicalcium salt are independently synthesized, and then coupled. Accordingly, related substances can be easily controlled and preparing time can be reduced, thus improving the productivity of a compound, and the yield of a final compound can also be increased.
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Paragraph 0100-0104
(2021/02/05)
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- Α-chloro -4 fluoro phenyl benzylone method for the synthesis of
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The invention relates to the field of chemistry, particularly to the field of medicinal chemistry, more particularly to a synthetic method for alpha-chlorine-4fluorine phenyl benzyl ketone, and aims to solve the problems that in the traditional preparation technology, the cost for preparing phenylacetic acid synthetic compound is high, the technology is complicated and the technology is not suitable for industrial production. The invention provides a novel synthetic method for alpha-chlorine-4fluorine phenyl benzyl ketone through adopting mandelic acid, which includes the following steps: alpha position chloro takes as the first step reaction, corresponding synthetic parameters are matched, and the mandelic acid takes as a starting material for synthesizing compound (4). Therefore, the total yield reaches 67.8% after three-step synthesis, by-products generated in the reaction are reduced, the purity of a target object is high, the purification is easy, and the method is suitable for industrial production.
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Paragraph 0032; 0033
(2017/04/28)
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- A PROCESS FOR PREPARATION OF 4-FLUORO-α-[2-METHYL-L-OXOPROPYL]-γ-OXO-N-β-DIPHENYLBENZENE BUTANE AMIDE
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A process for preparation of 4-fluoro-alpha-[2-methyl-l -oxopropyl]-gama-oxo-N- beta-diphenylbenzene butane amide also known as a diketone intermediate of atorvastatin, completely devoid of impurities 3,4-difluoro-alpha-[2-methyl-l-oxopropyl]-gama-oxo-n-beta-diphenylbenzene butane amide; methyl, 2 {-2[-(4-fluorophenyl)-2-oxo- 1 -phenyl ethyl)] } -4-methyl-3-oxo pentanoate; 1,4-bis(4-fluorophenyl)-2,3-diphenylbutane- 1,4-dione, 1 -(4-fluorophenyl)-2-phenyl ethanone; l-(4-fluorophenyl)-2-phenyl ethanone and containing about 0.05% or less of 2-methyl- l-oxopropyl]-gama-oxo-N-beta- diphenylbenzene butane amide. In that process the said diketone intermediate of formula 1 is obtained by maintaining temperature -25° C to 50° C during Friedel-Crafts acylation, in situ halogenation of formula II in presence of a solvent and nucleophilic substitution from a compound of formula III with formula IV in presence of a base.
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Page/Page column 19-20
(2012/11/07)
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- Azole derivatives
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Azole derivatives of the formula SPC1 Wherein R1 is free or esterified carboxyl or other functionally modified carboxyl group, R2 and R3 each are aryl; A is Cn H2n in which n is an integer from 1 to 10, inclusive; and Z is O or S; and the physiologically acceptable salts thereof, possess, with good compatibility, excellent antiphlogistic activity and, in particular, influence favorably the chronic progressive diseases of the joints, e.g., arthritis. They can be prepared from compounds of the formula SPC2 Wherein X1 is a group convertible into the group --S--A--R1, and R2 and R3 have the values given above.
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