CAS: 288-16-4; Isothiazole

该化合物是一种杂交循环化合物,其特点是五人环环,含有硫磺和氮原子;它是有机合成的多功能构件,特别是在开发药品,农用化学品和特殊化学品方面;其结构稳定性和反应性使其对建造生物活性分子,包括抗微生物剂和抗硫剂具有价值;Isothiazole衍生物也因其电子特性被用于材料科学.该化合物具有选择性的功能化能力,能够进行量身定制的修改,以满足具体应用要求.其在药用和工业化学方面的广泛用途凸显了其作为合成化学关键中间体的重要性.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

2-bromo-1,3-thiazole(5-chloro-2-nitro-phenyl)-isothiazol-5-yl-methanol 5-Acetyl-isothiazol 2-Benzyl-isothiazolium - Bromid (4-chloro-phenyl)-isothiazol-5-yl-methanol

合成工艺路线路线简述

    Thiosulfuric Acid S-(3-Oxo-Cis-Propenyl) Ester; Sodium Salt置于氨体系中,化学反应 2.0H,以60%的收率获得异噻唑
    参考文献:具有异噻唑并乙烯基侧链的新型1β-甲基卡宾烯的合成和生物学评估.
    标题:具有异噻唑并乙烯基侧链的新型1β-甲基卡宾烯的合成和生物学评估.
    摘要:描述了在吡咯烷环的c-5位置带有异噻唑并乙烯基的新型1β-甲基碳烯化合物1A,B的合成及其生物学评价.两种化合物均显示出有效且均衡的抗菌活性以及对dhp-1的高稳定性.特别是,与5-异恶唑衍生物2,亚胺培南和美洛培南相比,5-异噻唑衍生物1A表现出出色的dhp-1稳定性和先进的药代动力学特性.
    Doi:10.1016/s0960-894X(02)00948-4

    专利信息


    专利号:WO-2023233371-A1
    优先权日:2022-06-03
    标 题:A continuous flow process for synthesis of organic azides
    发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT
    权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE
    摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.

    专利号:US-12291596-B2
    优先权日:2018-11-30
    标 题 :Radical cascade-enabled synthesis of precision polymers with complex main-chain structures
    发明人:NIU JIA; HUANG HANCHU; WANG WENQI
    权利人:THE TRUSTEES OF BOSTON COLLEGE
    摘要:Radical cascade reactions enabling sequence-controlled ring-closing polymerization and ring-opening polymerization for the controlled synthesis of polymers with complex main-chain structures are provided. Facile syntheses leading to low-strain macrocyclic monomers consisting of the ring-opening triggers and extended main-chain structures are also provided. The present disclosure further provides methods for excellent control over polymer molecular weights and molecular weight distributions and high chain-end fidelity allows for the preparation of polymeric systems with well-defined architectures. Further provided are the general nature of the radical cascade-triggered transformations in polymer chemistry, and its application to the synthesis of polymers with diverse main-chain structural motifs with tailored functions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

    专利号:US-11161827-B2
    优先权日:2019-04-05
    标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination
    发明人:Zhang xiao-xiang; Lang kai
    权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE
    摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

    专利号:US-7160517-B2
    优先权日:2000-08-18
    标题 :Apparatus and methods for the automated synthesis of oligosaccharides
    发明人:SEEBERGER PETER H; PLANTE OBADIAH J
    权利人:MASSACHUSETTS INST OF TECHNOLG
    摘要:One aspect of the present invention relates to an apparatus for the efficient synthesis of oligosaccharides on a solid support, e.g., formed by subunit addition to terminal subunits immobilized on solid-phase particles. In certain embodiments, the apparatus of the present invention is used in combinatorial methods, e.g., as described herein, of synthesizing oligosaccharides.

    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-7230101-B1
    优先权日:2002-08-28
    标 题:Synthesis of methotrexate-containing heterodimeric molecules
    发明人:MURTHI KRISHNA K; SMITH CHASE C
    权利人:GPC BIOTECH INC
    摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
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    合成参考文献


    摘要:Nakao, Y., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 428.
    摘要:Zhang, H.; Liu, C.; Lei, A., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 144.
    参考文献:10.1016/s0960-894x(02)00338-4
    摘要:Clerici F, Gelmi ML, Yokoyama K, Pocar D, Van Voorhis WC, Buckner FS, Gelb MH. Isothiazole dioxides: synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase. Bioorganic & Medicinal Chemistry Letters. 2002 Aug;12(16):2217–20. doi: 10.1016/s0960-894x(02)00338-4.
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