CAS: 114-86-3; Phenformin

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CAS号834-28-6 盐酸苯乙双胍 | CAS号156-28-5 2-苯乙胺盐酸盐 | CAS号79246-47-2 4-AMINO-6-PHENE...

Phenformin Hydrochloride置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 2.0H,反应生成降糖灵
参考文献:一种5-氟尿嘧啶苯乙双胍盐的制备方法及晶体结构
标题:一种5-氟尿嘧啶苯乙双胍盐的制备方法及晶体结构
摘要:一种5‑氟尿嘧啶与苯乙双胍的盐,其制备方法及晶体结构,本发明涉及药物化学领域.该5‑氟尿嘧啶苯乙双胍盐的分子式为c14H18Fn7O2,由一个苯乙双胍阳离子与一个5‑氟尿嘧啶阴离子构成基本结构单元.该盐属于单斜晶系,空间群为p21/n.以5‑氟尿嘧啶原料药与苯乙双胍游离碱为原料,按摩尔比为1:1将两者混合溶解到甲醇与乙腈的混合溶剂中反应,以乙醇用作溶剂重结晶得到高纯度的5‑氟尿嘧啶苯乙双胍盐.本发明所述的5‑氟尿嘧啶苯乙双胍盐提高了5‑氟尿嘧啶的溶解性,有利于发挥5‑氟尿嘧啶与苯乙双胍的协同抗肿瘤活性.该盐结构中不存在任何结晶的溶剂分子,室温条件下长期放置仍能保持其晶体的骨架结构.

专利信息

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-8846916-B2
优先权日:2009-05-11
标题:Sitagliptin synthesis
发明人：GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH
权利人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH; GENERICS UK LTD
摘要:The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.

专利号:US-2008300418-A1
优先权日:2004-11-08
标 题:Synthesis of Cardiolipin Analogues and Uses Thereof
发明人：AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.

专利号:US-4286098-A
优先权日:1980-03-28
标 题:Process for the preparation of chiral hydantoins
发明人：SARGES REINHARD
权利人:PFIZER
摘要:A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. n The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.

专利号:US-4348526-A
优先权日:1980-03-28
标题:Intermediates in the preparation of chiral hydantoins
发明人：SARGES REINHARD
权利人:PFIZER
摘要:A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. n The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.

专利号:WO-2011103648-A1
优先权日:2010-02-23
标 题:Method for preparing ointments containing antioxidants from polyphenol-rich plants for use in the treatment of wounds of various origins which involve an increase in oxidation-promoting agents and/or increased formation of oxygen-derived reactive species and/or reduced formation of nitric oxide
发明人：SOARES DE MOURA ROBERTO
权利人:UNIV DO ESTADO DO RIO DE JANEIRO UERJ; SOARES DE MOURA ROBERTO
摘要:This invention relates to a method for producing oitnments and/or creams that contain antioxidants from polyphenol-rich plants such as Euterpe oleracea (assai palm), for use in the treatment of wounds, in order to accelerate the cicatrisation process, whenever there is an increase in the formation of oxidation-promoting compounds and a reduced synthesis of nitric oxide.