CAS: 40899-71-6; 1-(Phenylsulfonyl)-1H-Indole

上下游产品

CAS号120-72-9 吲哚 | CAS号98-09-9 苯磺酰氯 | CAS号81114-41-2 1-(苯磺酰)二氢吲哚 | CAS号99275-44-2 1-(benzenesulfo... | CAS号696-59-3 2,5-二甲氧基四氢呋喃 | CAS号98-10-2 苯磺酰胺 | CAS号1007561-82-1 3-hydroxy-1-phe... | CAS号26340-49-8 2-碘吲哚 | CAS号106154-54-5 1-(benzenesulfo... | CAS号83-34-1 3-甲基吲哚 | CAS号3469-20-3 2,3-二苯基吲哚 | CAS号249762-62-7 (5-hydroxy-1H-i... | CAS号25699-90-5 2-(1H-吲哚-1-基)苯甲腈 | CAS号26340-49-8 2-碘吲哚 | CAS号99655-68-2 3-溴-1-(苯基磺酰基)-1H-吲哚 | CAS号80360-14-1 1-苯磺酰基-3-碘吲哚 | CAS号80360-23-2 1-(苯磺酰)-1H-吲哚-2-甲醛 | CAS号5457-28-3 3-氰基吲哚

吲哚置于potassium Tert-Butylate,Sodium Hydroxide体系中,用 二氯甲烷,二甲基亚砜 作为反应溶剂,化学反应 37.0H,反应生成 N-苯磺酸吲哚
参考文献:无过渡金属和可见光介导的脱磺酰化和脱卤反应:Hantzsch酯阴离子作为电子和氢原子供体.
标题:无过渡金属和可见光介导的脱磺酰化和脱卤反应:Hantzsch酯阴离子作为电子和氢原子供体.
摘要:已开发出在室温(rt)和无过渡金属条件下进行n-和o-磺酰化的新方法.第一种方法涉及在室温下仅使用二甲基亚砜(dmso)中的ko T Bu将各种n-磺酰基杂环和苯基苯磺酸盐以非常好或优异的收率转化为相应的脱磺酰化产物.或者,已经使用可见光方法用作为可见光吸收剂的hantzsch酯(he)阴离子和电子和氢原子供体来促进n-甲基-N-芳基磺酰胺的脱保护,以促进脱磺酰化反应.he阴离子可轻松就地制备通过在室温下将相应的he与dmso中的ko T Bu反应.进一步研究了两种方案的合成范围和机制方面,以合理化脱磺酰化工艺的关键特征.此外,He阴离子在可见光照射下诱导芳基卤化物的还原脱卤反应.
DOI:10.1021/acs.Joc.0C01523

专利信息

专利号:US-5220016-A
优先权日:1991-07-29
标 题:Synthesis of navelbine analogs
发明人：MAGNUS PHILIP D; THURSTON LEE S
权利人:UNIV TEXAS
摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.

专利号:WO-2012088402-A1
优先权日:2010-12-22
标题 :Synthesis of conolidine and discovery of a potent non-opioid analgesic for pain
发明人：BOHN LAURA M; MICALIZIO GLENN C
权利人:SCRIPPS RESEARCH INST; BOHN LAURA M; MICALIZIO GLENN C
摘要:The first de novo synthetic pathway to the exceptionally rare C5-nor stemmadenine natural product, conolidine, and the first asymmetric synthesis of any member of this natural product class arc described. C5-nor stemmadenine compositions are also described. These compounds, for example,(+/- )-,(+)- and (-)-conolidine are potent and efficacious non-opioid analgesics in tonic and persistent pain.

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-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-2008281105-A1
优先权日:2005-01-18
标题:Novel Quinolinium Salts and Derivatives
发明人：MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE
权利人:IMMUSOL INC
摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.

专利号:US-11384076-B2
优先权日:2017-08-18
标 题:Synthesis, pharmacology and use of new and selective FMS-like tyrosine kinase 3 (FLT3) FLT3 inhibitors
发明人：MAHBOOBI SIAVOSH; SELLMER ANDREAS; PONGRATZ HERWIG; PILSL BERNARDETTE; KRÄMER OLIVER; KINDLER THOMAS; BEYER MANDY
权利人:UNIV REGENSBURG; UNIV DER JOHANNES GUTENBERG UNIV MAINZ
摘要:The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.