CAS: 90001-64-2; Benzo[b]Thiophene-2-Sulfonyl Chloride

该化合物是一种多用途的氯乙烯衍生物,用作有机合成中的关键中间体,特别是在制作磺酰胺和其他含硫化合物时;其反应式氯乙烯组能够高效地发挥功能,使其在制药和农用化学应用中具有价值;苯并硫苯核心提供了结构稳定性,提高了电益替代反应的回动性;该化合物在生物活性分子的合成中特别有用,因为它能够在温和条件下引进磺酰氟功能;高纯度和一贯性能确保研究和工业过程的可靠性;由于水分敏度和潜在的腐蚀性,需要妥善处理.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

Benzo[b]thiophene tert.-butyl lithium benzo[b]thiophene-2-sulfonamide benzo[b]thiophene-2-sulfonic acid [1-(3-cyano-benzyl)-2-oxo-pyrrolidin-3-(S)-yl]-amide benzo[b]thiophene-2-sulfonic acid (2-amino-phenyl)-amide Benzothiophene-2-sulfonic acid [1-(4-chloroquinolin-6-ylmethyl)-2-oxopyrrolidin-3-(S)-yl]-amide

合成工艺路线路线简述

  • 合成目标产物 1-Benzothiophene-2-Sulfonyl Chloride 主要起始原料 Thianaphthene
  • (文献来源)合成步骤主要原料 Thianaphthene
📜苯并噻吩置于正丁基锂,2,4,6-Trichlorophenyl Chlorosulfate体系中,用 四氢呋喃,2-甲基四氢呋喃,正己烷 作为反应溶剂,化学反应 4.0H,反应生成 1-苯并噻吩-2-磺酰氯
参考文献:由有机锌试剂和2,4,6-三氯苯基氯硫酸盐合成杂芳基磺酰胺
标题:由有机锌试剂和2,4,6-三氯苯基氯硫酸盐合成杂芳基磺酰胺
摘要:描述了一种使用2,4,6-三氯苯基氯硫酸盐(tcpc)制备芳基和杂芳基磺酰胺的方法.2-吡啶基锌试剂与tcpc的反应反应生成2,4,6-三氯苯基(tcp)吡啶-2-磺酸盐,并且母体吡啶-2-磺酸盐显示与胺反应.较少电子富集的芳基锌和杂芳基锌试剂与tcpc反应反应生成磺酰氯,该磺酰氯可就地转化为磺酰胺.
DOI:10.1021/acs.Orglett.5B01540

海关参考信息

专利信息


专利号:US-RE35279-E
优先权日:1987-08-28
标题:Hydantoin derivatives
发明人:MOCHIDA EI; MURAKAMI KIMIHIRO; KATO KAZUO; KATO KATSUAKI; OKUDA JUN; MIWA ICHITOMO
权利人:MOCHIDA PHARM CO LTD
摘要:The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

专利号:US-7411065-B2
优先权日:2002-04-26
标 题 :PNA monomer and precursor
发明人:KIM SUNG KEE; LEE HYUNIL; LIM JONG CHAN; CHOI HOON; JEON JAE HOON; AHN SANG YOUL; LEE SUNG HEE; YOON WON JUN
权利人:PANAGENE INC
摘要:This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oglimers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: n nwhereinn E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

专利号:US-5202339-A
优先权日:1987-08-28
标题:Hydantoin derivatives
发明人:MOCHIDA EI; MURAKAMI KIMIHIRO; KATO KAZUO; KATO KATSUAKI; OKUDA JUN; MIWA ICHITOMO
权利人:MOCHIDA PHARM CO LTD
摘要:The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives and pharmaceutical compositions containing at least one of hydantoin derivatives as hypoglycemic as well as hypolipidemic agents. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites. The compounds of the present invention represent a satisfactory hypoglycemic as well as hypolipidemic activity. These compounds are extremely useful for the treatment and/or prevention of diabetes mellitus with or without hyperlipidemia. It is indicated that the compounds of the present invention are useful for the treatment and/or prevention of diabetic complications such as somatic or autonomic neuropathy, cataract, retinopathy, nephropathy or microangiopathy. It is also indicated that the compounds of the present invention are useful for the treatment and/or prevention of hyperlipidemia.

专利号:US-4914099-A
优先权日:1987-08-28
标 题:Hydantoin derivatives as aldose reductase inhibitors
发明人:MOCHIDA EI; KATO KAZUO; KATO KATSUAKI; MIWA ICHITOMO; OKUDA JUN
权利人:MOCHIDA PHARM CO LTD
摘要:The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. n The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.

专利号:EP-0355827-B1
优先权日:1988-08-24
标 题:Hydantoin derivatives
发明人:MOCHIDA EI; MURAKAMI KIMIHIRO; KATO KAZUO; KATO KATSUAKI; OKUDA JUN; MIWA ICHITOMO A
权利人:MOCHIDA PHARM CO LTD
摘要:The present invention relates to hydantoin derivatives, represented by the formula (I): and non-toxic salts, solvates and solvates of non-toxic salts thereof; wherein q represents a mono- or a fused heterocyclic group which may be substituted by one or more substituents which are same or different and selected from a group consisting of a halogen atom, an alkyl group, a nitro group, a cyano group, an optionally protected carboxy group, an optionally protected carboxymethyl group, a halogenated alkyl group, an alkylthio group, an alkylcarbonyl group, an alkoxy group, an alkylsulfinyl group, an alkylsulfonyl group, an optionally protected hydroxy group, an optionally protected amino group, a carbamoyl group and a phenyl group, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and intermediate compounds in the synthesis of said hydantoin derivatives.

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