CAS: 1420477-60-6; (S)-4-(8-Amino-3-(1-(But-2-Ynoyl)Pyrrolidin-2-yl)Imidazo[1,5-A]Pyrazin-1-yl)-N-(Pyridin-2-yl)Benzamide

上下游产品

4-[8-氨基-3-(2S)-2-吡咯烷基咪唑并[1,5-A]吡嗪-1-基]-N-2-吡啶基苯甲酰胺 (S)-4-(8-Amino-3-(Pyrrolidin-2-yl)Imidazo[1,5-A]Pyrazin-1-yl)-N-(Pyridin-2-yl)Benzamide 1420478-90-5
中间体 (S)-Benzyl 2-(8-Amino-1-(4-(Pyridin-2-Ylcarbamoyl)Phenyl)Imidazo[1,5-A]Pyrazin-3-yl)Pyrrolidine-1-Carboxylate 1420478-89-2
(2S)-2-(8-氨基-1-溴咪唑并[1,5-A]吡嗪-3-基)-1-吡咯烷羧酸苯甲酯 (S)-Benzyl 2-(8-Amino-1-Bromoimidazo[1,5-A]Pyrazin-3-yl)Pyrrolidine-1-Carboxylate 1420478-88-1
(S)-苄基2-(1-溴-8-氯咪唑并[1,5-A]吡嗪-3-基)吡咯烷-1-羧酸 (S)-Benzyl 2-(1-Bromo-8-Chloroimidazo[1,5-A]Pyrazin-3-yl)Pyrrolidine-1-Carboxylate 1420478-87-0
阿卡布鲁替尼 (S)-Benzyl 2-(8-Chloroimidazo[1,5-A]Pyrazin-3-yl)Pyrrolidine-1-Carboxylate 1418307-18-2

(S)-2-{8-Tert-Butoxycarbonylamino-1-[4-(2-Pyridylcarbamoyl)Phenyl]Imidazo[1,5-A]Pyrazin-3-Yl}-1-(2-Butynoyl)Pyrrolidine置于三氟乙酸体系中,用 甲醇 用作溶剂,化学反应 6.0H,以92%的收率获得阿可替尼
参考文献:一种治疗慢性淋巴细胞白血病的btk抑制剂 Acalabrutinib的合成方法
标题:一种治疗慢性淋巴细胞白血病的btk抑制剂 Acalabrutinib的合成方法
摘要:一种治疗慢性淋巴细胞白血病的btk抑制剂acalabrutinib的合成方法,步骤:制备(S)‑2‑(8‑氨基咪唑并[1,5‑a]吡嗪‑3‑基)‑1‑吡咯烷甲酸苄酯;制备(S)‑2‑(8‑叔丁氧羰基氨基咪唑并[1,5‑a]吡嗪‑3‑基)‑1‑吡咯烷甲酸苄酯;制备(S)‑2‑(8‑叔丁氧羰基氨基‑1‑溴咪唑并[1,5‑a]吡嗪‑3‑基)‑1‑吡咯烷甲酸苄酯;制备(S)‑2‑{8‑叔丁氧羰基氨基‑1‑[4‑(2‑吡啶基氨甲酰基)苯基]咪唑并[1,5‑a]吡嗪‑3‑基}‑1‑吡咯烷甲酸苄酯;制备(S)‑2‑{8‑叔丁氧羰基氨基‑1‑[4‑(2‑吡啶基氨甲酰基)苯基]咪唑并[1,5‑a]吡嗪‑3‑基}吡咯烷;制备(S)‑2‑{8‑叔丁氧羰基氨基‑1‑[4‑(2‑吡啶基氨甲酰基)苯基]咪唑并[1,5‑a]吡嗪‑3‑基}‑1‑(2‑丁炔酰基)吡咯烷;制备acalabrutinib.收率高;简化流程;绿色环保.

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-2022073513-A1
优先权日:2018-12-29
标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases
发明人：CHEN YI
权利人:NEWAVE PHARMACEUTICAL INC
摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).

专利号:US-3717556-A
优先权日:1969-06-14
标 题 :PROCESS FOR THE PREPARATION OF beta -HALOGENO-ALKYL-ISOCYANATES
发明人：KAMPE K
权利人:HOECHST AG
摘要:N-halogeno-alkyl- Beta -lactams are rearranged into Beta halogeno-alkyl-isocyanates by contacting them with unsaturated organic compounds, optionally under irradiation. The products are highly reactive and useful for the synthesis of heterocyclic compounds.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

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.