噻唑置于正丁基锂,四溴化碳体系中,用 四氢呋喃 用作溶剂,化学反应 0.25H,以80%的收率获得2-溴噻唑 参考文献:Tetrahalogenomethanes: Simple Reagents For The Synthesis Of Monohalogenated And Mixed Dihalogenated Aromatic Heterocycles Via Metal-halogen Exchange From Lithium Compounds 标题:Tetrahalogenomethanes: Simple Reagents For The Synthesis Of Monohalogenated And Mixed Dihalogenated Aromatic Heterocycles Via Metal-halogen Exchange From Lithium Compounds 摘要:Tetrabromo-Or Tetrachloromethane And 2-Lithio Derivatives Of Aromatic Heterocycles Rapidly Produce The Corresponding 2-Bromo Or 2-Chloro Derivatives In High Yields Through A Metal-Halogen Exchange Mechanism. This Kind Of Reaction Was Also Used To Obtain,In Good Yields,5-Bromo-2-Chlorothiazole And 5-Bromo-2-Chloro-N-Methylimidazole. (C) 2000 Elsevier Science S.A. All Rights Reserved. Doi:10.1016/s0022-328X(00)00068-1
专利信息
专利号:US-6603015-B2 优先权日:1999-03-29 标题:Synthesis of epothilones 发明人:GEORG GUNDA I; NAIR SAJIV K; REIFF EMILY; TUNOORI ASHOK RAO 权利人:UNIV KANSAS 摘要:Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-11465997-B2 优先权日:2017-06-22 标 题 :Synthesis of disorazoles and analogs thereof as potent anticancer agents 发明人:NICOLAOU KYRIACOS C; BELLAVANCE GABRIEL; BUCHMAN MAREK; PULUKURI KIRAN KUMAR; RIGOL STEPHAN 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present disclosure provides disorazole analogs of the formula: 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-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-6774229-B2 优先权日:1999-11-21 标 题 :Coupling condensation synthesis of heterocycles 发明人:MUELLER THOMAS; ANSORGE MARKUS 权利人:MORPHOCHEM AG 摘要:The invention relates to a process for the preparation of heterocycles, characterised in that the following components: n i) a propargyl derivative of the general structural formula I n  a wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile; n (ii) a compound of the general structural formula II, n n n B—X  II, n n n  wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group; n (iii) a nucleophile of the general structural formula III, n n n Y—C n —Z  III, n n n  wherein Y and/or Z, each independently of the other, is an amino group, thio group (mercapto group), seleno group, telluro group, hydroxy group (alcohol group), imido group, carbonyl group, thiocarbonyl group, selenocarbonyl group, tellurocarbonyl group; C is a substituted or unsubstituted C atom, a substituted or unsubstituted or annelated CC double bond or single bond and n=0-10, preferably 1-5, preferably are reacted in a one-pot reaction by cyclocondensation to form 4- to 10-membered, preferably 5- to 7-membered, heterocyclic, aromatic or non-aromatic ring systems.
专利号:US-6457303-B1 优先权日:1999-03-29 标题:Synthesis of epothilones 发明人:GEORG GUNDA I; NAIR SAJIV K; REIFF EMILY; TUNOORI ASHOK RAO; HENRI JOHN T 权利人:UNIV KANSAS 摘要:Various epothilone precursors needed for the preparation of final epothilones are provided.
[参考文献]: Mohammed Al-Hashimi, Et Al. Synthesis And Characterization Of Fused Pyrrolo[3,2-D:4,5-D']Bisthiazole-Containing Polymers. Org Lett. 2010 Dec 3;12(23):5478-81.
合成参考文献
摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 66. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 355. 摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 470. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 346. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 192.