CAS: 2899-29-8; (S)-2-Amino-3-(1H-Indol-3-yl)Propan-1-Ol

上下游产品

L-tryptophan methyl ester (S)-tryptophan methyl ester hydr°Chloride L-Tryptophan benzyl (S)-(1-hydroxy-3-(1H-indol-3-yl)propan-2-yl)carbamate(S)-4-[(1H-indol-3-yl)methyl]oxazolidin-2-one (S,S)-((((2-(indol-3-yl)-1-(hydroxymethyl)ethyl)amino)carbonyl)-2-methylpropyl)(methyl)carbamic acid, phenylmethyl ester benzyl (S)-(1-hydroxy-3-(1H-indol-3-yl)propan-2-yl)carbamate (2S)-3-(2-Indolyl)-2-(tosylamino)propyl toluene-p-sulfonate

L-色氨酸置于sodium Tetrahydroborate,三甲基氯硅烷体系中,用 甲醇 用作溶剂,化学反应 1.0H,反应生成L-色氨醇
参考文献:侧基疏水性的增加大大改善了cyp3A4的利托那韦样抑制剂的效价.
标题:侧基疏水性的增加大大改善了cyp3A4的利托那韦样抑制剂的效价.
摘要:确定有效抑制药物代谢性细胞色素p450 3A4(cyp3A4)所需的结构决定簇可以帮助开发更安全的药物和更有效的药物增强剂.我们利用合理的抑制剂设计来解释利托那韦类似物的结构活性关系,利托那韦是一种作为药物增强剂销售的高效cyp3A4抑制剂.分析具有不同立体结构的r1侧基为苯基或萘,R2为吲哚或萘的化合物显示:(i)与r2-萘类似的化合物比r2-苯基/吲哚具有更紧密的结合力和更强的cyp3A4抑制力包含同行 (II)立体化学成为一个更重要的贡献因素,因为庞大的侧基限制了优化蛋白质-配体相互作用的能力;(III)r1 / R2构型与优先结合cyp3A4的关系很复杂,并且取决于侧基的功能性/相互作用和主链间距;(iv)三种抑制剂5A-B和7D优于利托那韦(ic50分别为0.055-0.085μm和0.130μm).
Doi:10.1016/j.Bmc.2020.115349

专利信息

专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人：ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

专利号:US-10040752-B2
优先权日:2015-08-24
标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof
发明人：MKRTCHYAN GNEL; YAO QINGWEI
权利人:CODY LABORATORIES INC
摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.

专利号:WO-2023284262-A1
优先权日:2021-07-13
标 题 :3,4-fused seven-membered heterocyclic oxindole, synthesis method therefor and application thereof
发明人：Li shuai-shuai; HU FANGZHI; Ding Zhanshuai; LI XINYAO
权利人:UNIV QINGDAO AGRICULTURAL
摘要:Disclosed is a 3,4-fused seven-membered heterocyclic oxindole, a synthesis method therefor and an application thereof. A structure of a 3,4-fused seven-membered nitrogen heterocyclic oxindole is provided in the present invention. A method for synthesizing same is also provided, comprising the following steps: reacting propargyl alcohol containing an isatin framework with a nucleophile under specific conditions to prepare a 3,4-fused seven-membered nitrogen heterocyclic oxindole. A pharmaceutical composition is provided in the present invention. Also provided in the present invention is an application of a 3,4-fused seven-membered nitrogen heterocyclic oxindole in the preparation of a drug for treating cancer. Provided in the present invention is a method for efficiently synthesizing 3,4-fused seven-membered nitrogen heterocyclic oxindoles having different structures. This is the first time achieving efficient synthesis of bioactive molecules containing both benzazepine and 3,4-fused heterooxidized oxindole structures on the basis of a hydrogen migration strategy.

专利号:US-2019002394-A1
优先权日:2015-08-24
标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof

专利号:US-7468375-B2
优先权日:2004-04-26
标题:Inhibitors of the HIV integrase enzyme
发明人：DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU
权利人:PFIZER
摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.

专利号:US-2017057909-A1
优先权日:2015-08-24
标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof