CAS: 1211441-98-3; 7-Cyclopentyl-N,N-Dimethyl-2-((5-(Piperazin-1-yl)Pyridin-2-yl)Amino)-7H-Pyrrolo[2,3-D]Pyrimidine-6-Carboxamide

上下游产品

4-(6-nitropyridin-3-yl)-piperazine-1-carboxylic acid tert-butyl ester7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide hemi succinate 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide succinate salt succinic acid

N,N‐dimethyl‐7‐cyclopentyl‐2‐{[5‐(4‐benzylpiperazin‐1‐yl)Pyridin‐2‐yl]Amino}‐7H‐pyrrolo[2,3‐d]Pyrimidine‐6‐carboxamide置于5%-Palladium/activated Carbon,氢气体系中,用 乙醇 用作溶剂,40.0~45.0 °C,300.01 Kpa 条件下,反应 4.0H,以93.7%的收率获得瑞博司可里布
参考文献:一种瑞博西尼的工业化制备方法
标题:一种瑞博西尼的工业化制备方法
摘要:本发明涉及一种瑞博西尼的工业化制备方法.该方法包括:N,N‑二甲基‑2,2‑二卤代‑4‑氰基正丁酰胺(ⅱ)和甲叉化试剂(ⅲ)缩合反应,制备式ⅳ化合物;然后使式ⅳ化合物和式ⅴ化合物缩合得到式ⅵ化合物;化合物ⅵ和卤代环戊烷经过n‑取代反应得到n,N‑二甲基‑7‑环戊基‑2‑{5‑[(4‑pg取代基哌嗪‑1‑基)吡啶‑2‑基]}氨基‑7H‑吡咯[2,3‑d]并嘧啶‑6‑甲酰胺(ⅷ),化合物ⅷ经脱pg取代基得到瑞博西尼.本发明方法原料价廉易得,工艺流程简便,操作安全,成本低.

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-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:WO-2022207788-A3
优先权日:2021-04-01
标 题 :Process for the preparation of ribociclib and pharmaceutically acceptable salts thereof
发明人：STANFEL URSA; BEZENSEK JURE; ZUPANCIC KATJA; ROBEK SPELA; BERGANT SIMONCIC ANA
权利人:KRKA D D NOVO MESTO
摘要:The invention relates to the synthesis of Ribociclib, and in particular to the synthesis of a 4-[6-[[7-cyclopentyl-6-(dimethylcarbamoyl)pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-pyridyl]-piperazine-1-carboxylate, which is an important intermediate in the synthesis of Ribociclib. Further, the invention relates to novel physiologically acceptable salts of Ribociclib.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

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:US-2023037284-A9
优先权日:2018-11-30
标题:Combination therapy of peptidomimetic macrocycles
发明人：GUERLAVAIS VINCENT; ANNIS DAVID ALLEN
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.