CAS: 62708-56-9; (2R,3R)-2,3-Bis(Benzoyloxy)Succinic Acid Hydrate

专利信息

专利号:US-2025197439-A1
优先权日:2022-03-18
标 题:Decarboxylative acetoxylation using mn(ii) or mn(iii) reagent for synthesis of 4'-acetoxy-nucleoside and use thereof for synthesis of corresponding 4'-(dimethoxyphosphoryl)methoxy-nucleotide
发明人：VAGLE KURT EDRIC; BHADURI SAYANTAN; YANG GUOHAN
权利人:DICERNA PHARMACEUTICALS INC
摘要:The present invention relates to the preparation of nucleic acids, nucleosides, nucleotides, and analogues thereof useful as potent and stable RNA interference agents. The present invention provides improved yields and avoids the use of lead tetraacetate for decarboxylative acetylation which decreases the overall cost of production by removing the need for lead remediation and offers a significant reduction in the environmental costs in production.

专利号:US-11767317-B1
优先权日:2020-06-30
标题:Methods of synthesizing enantiopure deuterium-enriched pioglitazone
发明人：NAVARRE LAURE FRANÇOISE VALÉRIE; JACQUES VINCENT; BOLZE SÉBASTIEN
权利人:POXEL SA
摘要:The invention provides methods of synthesis of enantiopure deuterium enriched R-pioglitazone with structure of compound (IV), or a pharmaceutically acceptable salt thereof: n nThe invention further provides chemical intermediates useful in the synthesis of compound (IV), and methods of synthesizing those intermediates.

专利号:US-8269023-B2
优先权日:2007-03-05
标题 :Process for preparation of duloxetine hydrochloride
发明人：SIYAN RAJINDER SINGH; GOHEL SUNIL KUMAR VINUBHAI; SINGH GIRIJ PAL
权利人:SIYAN RAJINDER SINGH; GOHEL SUNIL KUMAR VINUBHAI; SINGH GIRIJ PAL; LUPIN LTD
摘要:An improved process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following:n (i) preparation of racemic condensed compound (RS)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (4) by reaction of racemic hydroxy compound (2) with 1-fluoronaphthalene (3) in presence of a base such as sodamide, potassium amide or potassium bis(trimethylsilyl)amide (KHDMS) in polar aprotic solvent, (ii) optical resolution of racemic condensed compound (5a+5b) with di-benzoyl-L-tartaric acid (7, DBTA, R=H) or di-para-anisoyl-L-tartaric acid (7, DATA, R=OCH 3 ) to obtain crude (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine dibenzoyl tartarate salt (8a) or (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine di-p-anisoyl tartarate salt (9a) respectively, (iii) optionally purification of crude tartarate salts (8a or 9a) by crystallization, (iv) optionally purification of duloxetine hydrochloride (1) by crystallization and (v) racemization of undesired (R)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (5b) by treatment with base potassium bis(trimethylsilyl)amide (KHDMS) to obtain racemic mixture of condensed compounds (5a and 5b).

专利号:US-8476437-B2
优先权日:2008-08-27
标题:Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
发明人：KOTHARI HIMANSHU MADHUSUDAN; DAVE MAYANK GHANSHYAMBHAI; PANDEY BIPIN; SHUKLA BHAVIN SHRIPRASAD
权利人:KOTHARI HIMANSHU MADHUSUDAN; DAVE MAYANK GHANSHYAMBHAI; PANDEY BIPIN; SHUKLA BHAVIN SHRIPRASAD; CADILA HEALTHCARE LTD
摘要:The present invention relates to synthesis of β-amino acid derivatives of formula (I) and its salts of formula (Ia) by a novel process. The process comprises the reduction of a protected or unprotected prochiral β-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic β-amino compound is resolved to a pure stereoisomer of formula (I), specifically to (2R)-4-oxo-4-[3-Ctrifluoromethyl)-5,6-dihydrol[1,2,4]triazolo[4,3-alpyrazin-7(8H)-yl]-1-(2,4,4-trifluorophenyl)butan-2-amine. In an embodiment the invention disclosed polymorphic forms of formula (I), phosphate salt of formula (I) and also a Dibenzoyl-L-tartaric acid salt of formula (I).

专利号:EP-4493568-A1
优先权日:2022-03-18
标 题 :Decarboxylative acetoxylation using mn(ii) or mn(iii) reagent for synthesis of 4'-acetoxy- nucleoside and use thereof for synthesis of corresponding 4'-(dimethoxyphosphoryl)methoxy- nucleotide

专利号:WO-2023177866-A1
优先权日:2022-03-18
标题 :Decarboxylative acetoxylation using mn(ii) or mn(iii) reagent for synthesis of 4'-acetoxy- nucleoside and use thereof for synthesis of corresponding 4'-(dimethoxyphosphoryl)methoxy- nucleotide