22728-89-8Relevant articles and documents
PROCESS FOR THE PREPARATION OF (R)-4-(1-(6-(4-(TRIFLUOROMETHYL)BENZYL)-6-AZASPIRO[2.5]OCTANE-5-CARBOXAMIDO)-CYCLOPROPYL) BENZOIC ACID OR A SALT THEREOF
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Page/Page column 15-16, (2021/10/02)
The present invention provides a process for preparing (R)-6-(tert-butoxycarbonyl)-6- azaspiro[2.5]octane-5-carboxylic acid (SM1), said process comprising the step of: iv) converting a compound of formula (VII) into a compound of formula (VIII) using a Wittig reagent in a suitable solvent; v) reacting through the Makosza reaction the compound of Formula (VIII) using bromoform and a suitable base to obtain cyclopropane compound of Formula (IX); and vi) removing bromine atoms in the presence of a reducing agent and a base in an alcoholic solvent thus obtaining (SM1). The invention relates also to a process for the conversion of the compound (SM1) for preparing (R)- 4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid (IV) or a salt thereof. The salt is preferably the sodium salt, more preferably the polymorphic form A of sodium (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6- azaspiro[2.5]octane-5-carboxamido)-cyclopropyl) benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2θ ±0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9.
A 10th factor inhibitor and its preparation method and application (by machine translation)
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Paragraph 0233; 0234; 0235, (2016/10/08)
The invention relates to a 10th factor inhibitor and its preparation and application, the 10th factor inhibitor has the structure of formula I, the invention inhibitors to alpha-amino acid as a template, respectively through the amide, carbamate, or urea to the branched chain is formed by a series of novel structure of the compound, this kind of compound can be effectively with the 10th factor binding, prevent the formation of thrombus. (by machine translation)
A new kind of diseases and three water vial preparation method of compound
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Paragraph 0035; 0036; 0037, (2017/04/27)
The invention belongs to the field of drug synthesis and discloses a preparation method of a novel amoxicillin trihydrate. The preparation method is characterized in that dibenzothiazyl disulfide as a reaction reagent undergoes a reaction to produce an active ester intermediate, and the active ester intermediate and amoxicillin undergo a condensation reaction to produce a desired compound. The preparation method reduces reaction processes, improves a yield, adopts easily available raw materials, has small dependence on equipment, is conducive to large-scale production, has low reaction toxicity, has small influence on the environment, reduces a production cost, realizes product purity greater than 99% and realizes single impurity content less than 0.2%.