CAS: 10075-50-0; 5-Bromoindole

上下游产品

CAS号26807-69-2 1-乙酰基吲哚啉-2-磺酸钠 | CAS号877-03-2 5-溴吲哚-3-甲醛 | CAS号182344-70-3 5-溴-1H-吲哚-1-甲酸叔丁酯 | CAS号128373-13-7 1H-Indol-5-yl t... | CAS号105205-48-9 [(E)-2-(5-bromo... | CAS号118757-11-2 5-溴-1-(苯磺酰基)-1H-吲哚 | CAS号88131-63-9 5-bromo-1-methy... | CAS号22190-33-6 5-溴吲哚啉 | CAS号918529-91-6 1H-Indole-1-car... | CAS号61-50-7 N,N-二甲基色胺 | CAS号32774-29-1 5-溴色醇 | CAS号400071-95-6 1-甲基-5-溴-3-吲哚甲酸 | CAS号475102-13-7 N-B°C-5-溴吲哚-2-硼酸 | CAS号32996-16-0 吲哚-5-甲酸乙酯 | CAS号143724-34-9 5-三丁基锡-1H-吲哚 | CAS号144104-44-9 5-(4-氟苯基)-1H-吲哚 | CAS号17422-32-1 5-氯吲哚 | CAS号90271-86-6 5-溴-3-氰基吲哚 | CAS号40432-84-6 5-溴吲哚-3-乙酸

N-Tosyl-5-Bromoindole置于sodium Hydride体系中,用 N,N-二甲基乙酰胺 用作溶剂,化学反应 1.0H,以92%的收率获得5-溴吲哚
参考文献:Nah促进的各种对甲苯磺酰胺的n-脱甲苯基化反应
标题:Nah促进的各种对甲苯磺酰胺的n-脱甲苯基化反应
摘要:据报道,由nah介导的各种ts保护的吲哚,氮杂杂环,苯胺和二苄基胺的解毒反应.该方法试剂便宜,操作方便,反应条件温和,底物范围广.此外,这项研究表明,由于可能发生不利的脱甲苯基作用,因此应控制在含氮化合物以nah为碱的含氮化合物甲苯磺酸化反应中nah的负载量.
Doi:10.1016/j.Tetlet.2020.152442

专利信息

专利号:US-8426612-B2
优先权日:2009-04-22
标 题:Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole
发明人：SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO
权利人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO; ITALIANA SINT SPA
摘要:The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.

专利号:WO-2011024039-A1
优先权日:2009-08-25
标题 :Synthesis of novel 5-(2-(phenylsulfonyl)ethyl)-1h-indole derivatives
发明人：POTLURI RAMESH BABU; KODALI HARI PRASAD; VENTURI SRINIVASA RAO; TADIMALLA VENKATA SRIHARI
权利人:POTLURI RAMESH BABU; KODALI HARI PRASAD; VENTURI SRINIVASA RAO; TADIMALLA VENKATA SRIHARI
摘要:An objective of the present invention is to develop commercially viable methods for the synthesis of 5-[2-phenylsulfony)ethyl]-1H-indole of Formule (II), where R 1 and R 2 are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (II). Another objective of the present invention is to convert the product Formula (II) to Formula (I) in high yields, where R 1 and R 2 are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (I). One of the first processes attempted was by reacting the indole derivative of Formula (III) with aryl vinyl sulphones of Formula (V) as shown in Scheme-III. Another process attempted was by reacting the aniline derivative of Formula (VI) with aryl sulphones of Formula (VII) as shown in Scheme-III. Scheme IV.

专利号:US-6303764-B1
优先权日:1998-09-24
标题:Synthesis of 4,7-dialkyl chromogenic glycosides of N-acetylneuraminic acids
发明人：SRIVASTAVA OM; SRIVASTAVA GEETA; DU MINGHUI; HINDSGAUL OLE; BUNDLE DAVID R; LIAV AVRAHAM
权利人:ZYMETX INC; HALIFEX FUND L P
摘要:The present invention provides an improved method of preparing a 4,7-di-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in detecting influenza virus types A and B. The ketosides are substrates that are selectively cleaved by a neuraminidase on influenza virus, but not be neuraminidases found on other viruses or on bacteria. The synthesis is efficient and provides large quantities of the ketoside for commercial development. The synthesis includes a step of alkylating the 4- and 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by a process that comprises contacting the derivative with a composition comprising an alkyl halide to form a 4,7-di-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The synthesis alternatively includes protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.

专利号:US-7652137-B2
优先权日:2003-03-06
标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines
发明人：GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH
权利人:EISAI R&D MAN CO LTD
摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.

专利号:US-2023220001-A1
优先权日:2020-06-09
标 题:Method for synthesis of thioether-containing peptides
发明人：GRUSS HENDRIK; LUTZ CHRISTIAN; SÃœSSMUTH RODERICH; Yao guiyang; KNITTEL CAROLINE; KOSOL SIMONE; MAINZ ANDI
权利人:HEIDELBERG PHARMA RES GMBH
摘要:The present invention relates to a method of formation of a sulphur bridge between tryptophan and cysteine in solid phase peptide synthesis under iodine treatment. The invention also relates to the resulting compounds of the method and their respective use.

专利号:US-9969686-B2
优先权日:2014-08-05
标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.