CAS: 1297538-32-9; N-((S)-1-(3-(3-Chloro-4-Cyanophenyl)-1H-Pyrazol-1-yl)Propan-2-yl)-5-(1-Hydroxyethyl)-1H-Pyrazole-3-Carboxamide

上下游产品

(S)-5-Acetyl-N-(1-(3-(3-Chloro-4-Cyanophenyl)-1H-Pyrazol-1-yl)Propan-2-yl)-1H-Pyrazole-3-Carboxamide 1297537-33-7
乾平 (S)-4-(1-(2-Aminopropyl)-1H-Pyrazol-3-yl)-2-Chlorobenzonitrile 1297537-41-7
2-氯-4-(1-(四氢-2H-吡喃-1H-吡唑-5-基)苯腈 2-Chloro-4-(1-(Tetrahydro-2H-Pyran-2-yl)-1H-Pyrazol-5-yl)Benzonitrile 1297537-35-9

1-(5-((S)-1-(3-(3-Chloro-4-Cyanophenyl)-1H-Pyrazol-1-yl)Propan-2-Yl-Carbamoyl)-1H-Pyrazol-3-yl)Ethyl Acetate置于sodium Hydroxide体系中,用 乙醇,水 用作溶剂,以93.3%的收率获得达若鲁胺
参考文献:一种多拉米胺的合成方法
标题:一种多拉米胺的合成方法
摘要:本发明提供了一种多拉米胺的合成方法,包括将4‑乙酰基‑2‑氯苯腈和dmf.dma反应得到化合物式2,然后通过两种方法合成出化合物式6:再经脱boc成盐,缩合,脱保护等步骤得到多拉米胺化合物式10;该合成方法不仅大大缩短了合成路线,极大地提高了路线效率,并降低了工艺成本,而且减少了副产物的生成,利于提高最终成品纯度,适合放大生产.反应式如下所示:

专利信息

专利号:US-2023391824-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
发明人：JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL
权利人:NARENDRAN ARUMUGAVADIVEL
摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

专利号:US-11491246-B2
优先权日:2020-07-13
标 题:Radiopharmaceutical and methods
发明人：MCCANN JOE
权利人:POINT BIOPHARMA INC
摘要:The radiopharmaceutical 177 Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of 177 Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise 177 Lu-PSMA I&T.

专利号:US-11129912-B1
优先权日:2020-07-13
标 题 :Radiopharmaceutical and methods
发明人：MCCANN JOE
权利人:POINT BIOPHARMA INC
摘要:The radiopharmaceutical 177Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of 177Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise 177Lu-PSMA I&T.

专利号:CN-111116477-A
优先权日:2019-12-27
标 题 :Synthesis of Dolaminamine

专利号:CA-2192366-A1
优先权日:1994-06-08
标 题:Genes for the synthesis of antipathogenic substances