CAS: 283173-50-2; 8-Fluoro-2-(4-((Methylamino)Methyl)Phenyl)-4,5-Dihydro-1H-Azepino[5,4,3-Cd]Indol-6(3H)-One

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CAS号880160-69-0 [4-(8-fluoro-6-... | CAS号773059-19-1 Rucaparib inter... | CAS号283173-84-2 4-(8-氟-3,4,5,6-... | CAS号283172-68-9 WD2000-012547 | CAS号1408282-25-6 3-(2-(1,3-二氧代异吲... | CAS号1408282-26-7 8-氟-1,3,4,5-四氢-... | CAS号283173-80-8 2-溴-8-氟-1,3,4,5...

[4-(8-Fluoro-6-Oxo-3,4,5,6-Tetrahydro-1H-Azepino[5,4,3-Cd]Indol-2-yl)-Benzyl]-Methyl-Carbamic Acid Methyl Ester置于氢溴酸,溶剂黄146体系中,化学反应 12.0H,以89.7%的收率获得瑞卡帕布
参考文献:治疗卵巢癌药物瑞卡帕布的制备方法
标题:治疗卵巢癌药物瑞卡帕布的制备方法
摘要:本发明公开一种治疗卵巢癌药物rucaparib的制备方法,该制备方法包括:步骤一,化合物a与带pg保护基的化合物b在缚酸剂的作用下,在有机溶剂a中发生酰化反应,制备得到式i化合物;步骤二,所述式i化合物在含水有机溶剂b中在酸c的作用下水解烯胺键,得式ii化合物;步骤三,所述式ii化合物在还原剂的作用下还原硝基为氨基后,脱水环合为式iii化合物;步骤四,所述式iii化合物与n‑(2‑乙醛基)邻苯二甲酰亚胺在酸d的作用下,缩合得式iv化合物;步骤五,所述式iv化合物脱除邻苯二甲酰保护基的同时环合得式v化合物;步骤六,所述式v化合物脱除所述pg保护基得rucaparib.本发明降低了治疗卵巢癌药物rucaparib的生产成本.

专利信息

专利号:WO-2022238500-A1
优先权日:2021-05-12
标题 :Radiosynthesis of [18f] talazoparib
发明人：BOWDEN GREGORY DAVID; MAURER ANDREAS; STOTZ SOPHIE; KINZLER PAUL JOHANNES OSKAR MARIA; LAEMMERHOFER MICHAEL; ZENDER LARS; PICHLER BERND
权利人:UNIV TUEBINGEN MEDIZINISCHE FAKULTAET
摘要:The present invention relates to the synthesis of Poly (ADP ribose) polymerase (PARP) inhibitors and particularly to the radiosynthesis of PARP 1 inhibitors, more particularly to the synthesis of [18F] talazoparib.

专利号:US-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人：ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.

专利号:WO-2019020508-A1
优先权日:2017-07-26
标 题 :PROCESS FOR THE PREPARATION OF HIGH-PURITY RUCAPARIB
发明人：BELOGI GIANLUCA; MAZZONI ANDREA; SERRA STEFANO; NOVO BARBARA
权利人:OLON SPA
摘要:The present invention relates to a new low environmental impact method for the synthesis of rucaparib with high yield and purity, said process comprising a regioselective coupling reaction between indole and iodo-aryl, carried out in water in the presence of a catalyst. The process of the invention is industrially advantageous because in the key coupling step, high regioselectivity is achieved without the use of complex intermediates or potentially toxic and environmentally harmful solvents.

专利号:US-11801232-B2
优先权日:2019-11-27
标 题 :Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
发明人：HUANG GLORIA
权利人:UNIV YALE
摘要:This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.

专利号:US-9993570-B2
优先权日:2014-01-05
标题:Radiolabeled tracers for poly (ADP-ribose) polymerase-1 (PARP-1), methods and uses therefor
发明人：MACH ROBERT; CHU WENHUA; ZHOU DONG; MICHEL LOREN; CHEN DELPHINE
权利人:UNIV WASHINGTON
摘要:Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [ 18 F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [ 18 F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.

专利号:US-2025127768-A1
优先权日:2022-06-30
标 题:Therapeutic targeting of inositol pyrophosphate synthesis in cancer
发明人：GOLUB TODD; BONDESON DANIEL
权利人:BROAD INST INC
摘要:The subject matter disclosed herein is generally directed to treating cancers sensitive to phosphate dysregulation with inhibitors of inositol pyrophosphate (PP-InsP) synthesis, in particular, inhibitors of inositol hexakisphosphate kinases IP6Ks.