CAS: 220438-80-2; 4-(Carboxymethyl)-2-Ethoxybenzoic Acid (Repaglinide Impurity)

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CAS号50-85-1 4-甲基水杨酸 | CAS号88709-17-5 2-乙氧基-4-甲基苯甲酸乙酯 | CAS号110017-07-7 ethyl 4-bromome... | CAS号332347-69-0 2-乙氧基-4-乙氧基羰基甲基...

📜4-甲基水杨酸置于盐酸,N-溴代丁二酰亚胺(Nbs),偶氮二异丁腈,苄基三丁基氯化铵,Potassium Carbonate,Sodium Nitrite体系中,用 四氯化碳,乙醚,二氯甲烷 用作溶剂,化学反应 76.5H,反应生成(4-羧基-2-乙氧基-苯基)-乙酸
参考文献:瑞格列奈和相关的降血糖苯甲酸衍生物.
标题:瑞格列奈和相关的降血糖苯甲酸衍生物.
摘要:研究了两个系列的降血糖苯甲酸衍生物(5,6)的构效关系.当2-甲氧基被亚烷基亚氨基残基取代时,系列5由美格替宁(3)产生.用顺式3,5-二甲基哌啶子基(5H)和八亚甲基亚氨基(5L)残基观测到最大活性.当将2-甲氧基,5-氟和α-甲基残基替换为2-哌啶子基,5-氢和较大的α-烷基残基时,具有反向酰胺基功能的meglitinide类似物4产生6系列,分别.羧基邻位的烷氧基残基进一步增加了大鼠的活性和作用时间.最具活性的外消旋化合物6Al(r4 =异丁基; R =乙氧基)的活性比磺酰脲(su)格列本脲(1)高12倍.发现活性主要存在于(S)-对映异构体中.与sus 1和2(格列美脲)相比,活性最高的对映异构体(S)-6Al(ag-Ee 623 Zw;瑞格列奈; Ed50 = 10 Micro / Kg Po)活性高25和18倍.瑞格列奈对2型糖尿病患者是一种有用的治疗药物.Fda和emea最
Doi:10.1021/jm9810349

专利信息

专利号:US-8198054-B2
优先权日:2007-01-22
标题 :Method for the chemo-selective enzymatic hydrolysis if a diester compound for preparing a monoester monoacid compound
发明人：BURGOS ALAIN; CAILLE JEAN-CLAUDE; LORRAINE-GRADLEY MICHELLE
权利人:BURGOS ALAIN; CAILLE JEAN-CLAUDE; LORRAINE-GRADLEY MICHELLE; ZACH SYSTEM; NOVACTA BIOSYSTEM LTD
摘要:This disclosure relates to the synthesis of the compound of formula (I) according to Scheme A below: n nin which R1, R2 and R3, which may be identical or different, represent, individually and independently, an alkyl group, characterized by an enzymatic hydrolysis reaction that involves placing the compound of formula (II) in contact with an enzyme that performs a chemoselective hydrolysis of only one of the two ester functions of the compound of formula (II) to obtain the compound of formula (I).