CAS: 1351636-18-4; (R)-6-Amino-9-(1-(But-2-Ynoyl)Pyrrolidin-3-yl)-7-(4-Phenoxyphenyl)-7,9-Dihydro-8H-Purin-8-One

结构式图片

欧盟法规

C&L通报

上下游产品

(R)-6-Amino-7-(4-Phenoxyphenyl)-9-(Pyrrolidin-3-yl)-7H-Purin-8(9H)-One 1351636-75-3
Tert-Butyl (3R)-3-[6-Amino-8-Oxo-7-(4-Phenoxyphenyl)-7,8-Dihydro-9H-Purin-9-Yl]Pyrrolidine-1-Carboxylate
Tert-Butyl (3R)-3-[6-(Benzylamino)-8-Oxo-7-(4-Phenoxyphenyl)-7,8-Dihydro-9H-Purin-9-Yl]Pyrrolidine-1-Carboxylate
Tert-Butyl (3R)-3-[6-Chloro-8-Oxo-7-(4-Phenoxyphenyl)-7,8-Dihydro-9H-Purin-9-Yl]Pyrrolidine-1-Carboxylate
Tert-Butyl (3R)-3-[6-(Dibenzylamino)-8-Oxo-7,8-Dihydro-9H-Purin-9-Yl]Pyrrolidin-1-Carboxylate
Tert-Butyl (3R)-3-(6-Amino-8-Oxo-7,8-Dihydro-9H-Purin-9-yl)Pyrrolidine-1-Carboxylate

合成工艺路线路线简述

  • 合成目标产物 Btk Kinase Inhibitor 主要起始原料 1-Pyrrolidinecarboxylic Acid, 3-[[6-[bis(Phenylmethyl)Amino]-5-Nitro-4-Pyrimidinyl]Amino]-, 1,1-Dimethylethyl Ester, (3R)-
  • (文献来源)合成步骤主要原料 1-Pyrrolidinecarboxylic Acid, 3-[[6-[bis(Phenylmethyl)Amino]-5-Nitro-4-Pyrimidinyl]Amino]-, 1,1-Dimethylethyl Ester, (3R)-
📜N-(4,6-Dichloropyrimidin-5-yl)-N-(4-Phenoxyphenyl)Formamide置于n-甲基吗啉,盐酸,1-丙基磷酸酐,1,8-二氮杂双环[5.4.0]十一碳-7-烯,三乙胺体系中,用 甲醇,水,乙酸乙酯,异丙醇,甲苯,乙腈 用作溶剂,2.0~115.0 °C,300.01 Kpa 条件下,反应 24.5H,反应生成替拉鲁替尼
参考文献:Process For Producing Purinone Derivative
标题:Process For Producing Purinone Derivative
摘要:根据本发明,与众所周知的生产方法不同,通过使用不同的起始物质,可以避免随着生产规模的增加而可能降低产量的乌尔曼缩合反应,从而可以安全稳定地提供6-氨基-9-[(3R)-1-(2-丁炔酰基)-3-吡咯啉基]-7-(4-苯氧基苯基)-7,9-二氢-8H-嘌呤-8-酮,并获得高反应产率.

海关参考信息

专利信息


专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人:EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Yu H, Truong H, Mitchell SA, Liclican A, Gosink JJ, Li W, Lin J, Feng JY, Jürgensmeier JM, Billin A, Xu R, Patterson S, Pagratis N. Homogeneous BTK Occupancy Assay for Pharmacodynamic Assessment of Tirabrutinib (GS-4059/ONO-4059) Target Engagement. SLAS Discov. 2018 Oct;23(9):919-929. doi: 10.1177/2472555218786165. Epub 2018 Jul 16.
2: Munakata W, Ando K, Hatake K, Fukuhara N, Kinoshita T, Fukuhara S, Shirasugi Y, Yokoyama M, Ichikawa S, Ohmachi K, Gion N, Aoi A, Tobinai K. Phase I study of tirabrutinib (ONO-4059/GS-4059) in patients with relapsed or refractory B-cell malignancies in Japan. Cancer Sci. 2019 May;110(5):1686-1694. doi: 10.1111/cas.13983. Epub 2019 Mar 28.
3: Rule SA, Cartron G, Fegan C, Morschhauser F, Han L, Mitra S, Salles G, Dyer MJS. Long-term follow-up of patients with mantle cell lymphoma (MCL) treated with the selective Bruton's tyrosine kinase inhibitor tirabrutinib (GS/ONO-4059). Leukemia. 2020 May;34(5):1458-1461. doi: 10.1038/s41375-019-0658-7. Epub 2019 Dec 11.

合成参考文献


参考文献:10.1371/journal.pone.0171221
摘要:Yahiaoui A, Meadows SA, Sorensen RA, Cui Z, Keegan KS, Brockett R, Chen G, Quéva C, Li L, Tannheimer SL. PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors. PLoS ONE. 2017 Feb 08;12(2):e0171221. doi: 10.1371/journal.pone.0171221.
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