肼基甲酸甲酯置于盐酸,Potassium Carbonate体系中,用 乙醇,水,甲醇 用作溶剂,化学反应 4.25H,以39.3%的收率获得5-氨基-吡唑-3-甲酸乙酯 参考文献:Pyrazolopyrimidines,A Process For Their Preparation And Their Use As Medicine 标题:Pyrazolopyrimidines,A Process For Their Preparation And Their Use As Medicine 摘要:取代吡唑并嘧啶衍生物的公式(I) 其中 R1代表氯或溴; R2,R3,R4,R5,R6和r7独立代表例如氢或c1-6-烷基; R8代表r9的基团或r10的基团,其中两个r8基团之一代表r9,另一个r8基团代表ret;R9代表例如苯基或噻吩基团,R10代表例如氢或甲基; 是有效的mglur5调节剂,可用于预防急性和慢性神经障碍.
专利信息
专利号:WO-2006127595-A1 优先权日:2005-05-23 标题:5-aminopyrazole carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof 发明人:SKINNER PHILIP J; SEMPLE GRAEME; WEBB PETER 权利人:ARENA PHARM INC; SKINNER PHILIP J; SEMPLE GRAEME; WEBB PETER 摘要:The present invention relates to certain pyrazole carboxylic acid or ester derivatives of Formula (I) and pharmaceutically acceptable salts thereof which exhibit useful pharmacological properties, for example, as agonists for the GPCR referred to herein as RUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, such as, dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
专利号:CN-103073549-A 优先权日:2012-09-07 标题 :Synthesis of 3-bromopyrazoline[1,5-α]pyrimidine-2-carboxylic acid