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 convenient method of preparation arab League throws cillin sodium
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Paragraph 0031; 0032, (2016/10/10)
The invention discloses a convenient method for preparing aspoxicillin sodium. The method comprises the steps of adding D-aspartic acid into a mixed solution of thionyl chloride and methanol, reacting to prepare D-aspartic acid methyl ester hydrochloride, reacting the D-aspartic acid methyl ester hydrochloride with an aqueous solution of methylamine to obtain aspartic formamide, protecting the first amino on the aspartic formamide by using trifluoroacetyl, then reacting the aspartic formamide with carbonyldimidazole to form an active mixed acid anhydride, condensing the active mixed acid anhydride with an amoxicillin triethylamine salt, finally removing the protective ground and forming a sodium salt under the alkali condition to obtain a crude aspoxicillin product of the target product, and refining the crude product to obtain the high-purity aspoxicillin sodium finished product. The method has the advantages that the reagents are cheap, readily available and low in toxicity and environmental pressure, the process operation is compact and stable, the purity of the product is high and the like.
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)