CAS: 5398-36-7; Ethyl 2-Aminothiazole-4-Carboxylate

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Ethyl 2-Amino-1,3-Thiazole-4-Carboxylate Hydrobromide 以 二氯甲烷 作为反应溶剂,化学反应生成 2-氨基噻唑-4-甲酸乙酯
参考文献:噻唑基肽抗生素ge2270 A的简明全合成.
标题:噻唑基肽抗生素ge2270 A的简明全合成.
摘要:由n-叔丁氧羰基保护的缬氨酸以最长的20步线性序列合成了有效的抗生素噻唑基肽ge2270 A,总产率为4.8%.关键策略是通过从2,6-二溴-3-碘吡啶开始的连续交叉偶联反应组装2,3,6-三取代吡啶核.通过3-锌的2,6-二溴吡啶的negishi交叉偶联将完整的southern片段安装在三噻唑的2-碘噻唑末端(87%).在通过另一个negishi交叉偶联金属化成锌试剂后,以截短的2-溴噻唑-4-羧酸叔丁酯形式引入代表分子北部的c-6处的取代基.整个序列的决定性步骤是将大环化成29元大环内酰胺,这是通过发生在吡啶核的c-2处的分子内stille交叉偶联进行的,以75%的收率提供所需的产物.通过在代表ge2270 A东部的复杂二噻唑片段与3,6-二取代的2-溴吡啶之间的酰胺键形成(87%)获得所需的锡烷.最终步骤包括将丝氨酸-脯氨酸酰胺二肽附着到分子的北部(65%),形成恶唑啉环和甲硅烷基醚脱保护(总体占55%).
DOI:10.1002/chem.200701823

专利信息

专利号:EP-3686190-A1
优先权日:2013-07-11
标 题 :Synthesis of therapeutically active compounds

专利号:US-10874646-B2
优先权日:2015-10-16
标 题 :Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof
发明人：NICOLAOU KYRIACOS C; RHOADES DEREK; WANG YANPING; TOTOKOTSOPOULOS SOTIRIOS
权利人:UNIV RICE WILLIAM M
摘要:In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.

专利号:US-2008139558-A1
优先权日:2006-02-24
标题 :Quinolones useful as inducible nitric oxide synthase inhibitors
发明人：SMITH NICHOLAS D; ROPPE JEFFREY R; BONNEFOUS CELINE; PAYNE JOSEPH E; ZHUANG HUI; CHEN XIAOHONG; LINDSTROM ANDREW K; DURON SERGIO G; HASSIG CHRISTIAN A; NOBLE STEWART A
权利人:KALYPSYS INC
摘要:The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.

专利号:US-9550757-B2
优先权日:2010-03-05
标题:Nuclear transport modulators and uses thereof
发明人：SHACHAM SHARON; KAUFFMAN MICHAEL; SANDANAYAKA VINCENT P; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

专利号:CN-117777051-A
优先权日:2023-12-13
标 题:A kind of synthesis method of 2-bromo-5-chlorothiazole-4-carboxylate

专利号:WO-2017066606-A1
优先权日:2015-10-16
标题 :Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof