相似化合物
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ECHA物质C&L通报合成工艺路线路线简述
- 合成目标产物 Bicyclo[1.1.1]Pentan-3-Amine,Hydrochloride 主要起始原料 Bicyclo[1.1.1]Pentane-1-Carboxylic Acid
- (文献来源)合成步骤主要原料 Bicyclo[1.1.1]Pentane-1-Carboxylic Acid
1-Azidobicyclo[1.1.1]Pentane置于盐酸,三苯基膦体系中,用 四氢呋喃,水 用作溶剂,化学反应 3.0H,以35.5 Mg的收率获得1-双环[1,1,1]戊胺盐酸
参考文献:从1-叠氮基-3-碘代双环[1.1.1]戊烷合成双环[1.1.1]戊丹-1-胺的新途径
标题:从1-叠氮基-3-碘代双环[1.1.1]戊烷合成双环[1.1.1]戊丹-1-胺的新途径
摘要:从药物化学的观点来看,双环[1.1.1]戊丹-1-胺(1)已经用作独特且重要的部分.但是,从合成上讲,该化合物几乎没有受到关注,并且仅证明了一种可扩展的途径来制备该胺.减少易获得且可能通用的中间体1-Azido-3-Iodobicyclo [1.1.1]戊烷(2),可以为该目标提供灵活且可扩展的替代方案.在这里,我们描述了我们对这种难以捉摸的转变的审查,并报告了我们在这项努力中取得的成功.
Doi:10.1021/ol500635P
专利信息
专利号:WO-2025077835-A1
优先权日:2023-10-12
标 题 :Method for preparing monosubstituted bicyclo[1.1.1] pentane derivative
发明人:ROBERTSON JEREMY; Xiong Ziyue
权利人:OXFORD UNIV SUZHOU SCIENCE & TECHNOLOGY CO LTD
摘要:Provided in the present invention is a method for preparing a compound of formula V, which is characterized by comprising steps (S1) and (S2). (S1) Reacting a compound of formula II with a compound of a formula III to obtain a compound of formula IV; and (S2) reacting the compound of formula IV obtained in step (S1) with an electrophilic reagent to obtain a compound of formula V, wherein R1, R2, R3, R4 and R5 are independently selected from hydrogen or C1-20alkyl, or a group which at least breaks a bond between an aromatic ring and carbonyl, and wherein, R6 is hydrogen. The raw materials required by the synthesis method according to the present invention are commercially available, the reaction steps are simple and easy to operate, and the synthesis method is safe and efficient and can be used for industrial scale-up production.
专利号:EP-3848356-A1
优先权日:2020-01-07
标 题 :Aryl-n-aryl derivatives for treating a rna virus infection
权利人:ABIVAX; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER; INST CURIE
摘要:The present invention relates to a compound of formula (I):n nwherein: n X 2 represents a -CO-NR k - group, a -NR' k -CO- group, a -O- group, a -CO- group, a -SO 2 -group, a -CS-NH- group, a -CH 2 -NH-, an ngroup, or a heterocyclyl, wherein the heterocyclyl is a 5- or 6-membered ring comprising 1, 2, 3 or 4 heteroatoms selected from O, S and/or N; Y 2 represents a hydrogen atom, a halogen atom, a hydroxyl group, a morpholinyl group, optionally substituted by a (C 1 -C 4 )alkyl group or a trifluoromethyl group, a bridged morpholinyl group, a bridged bicycloalkyl group, a piperidinyl group, a (C 1 -C 4 )alkenyl group, a -PO(OR a )(OR b ) group, or a -CR 1 R 2 R 3 group, or any of its pharmaceutically acceptable salt. n The present invention further relates to new compounds, to pharmaceutical compositions containing them and to synthesis process for manufacturing them.
专利号:US-8080556-B2
优先权日:2008-08-13
标 题 :2-amino pyrimidine compounds as potent HSP-90 inhibitors
发明人:KUNG PEI-PEI; MENG JERRY JIALUN
权利人:KUNG PEI-PEI; MENG JERRY JIALUN; PFIZER
摘要:The present invention is directed to compounds of formula (I), n nor pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.
专利号:EP-2118111-B1
优先权日:2007-02-06
标题 :2-amin0-5, 7-dihydr0-6h- pyrrolo [3, 4-d] pyrimidine derivatives as hsp-90 inhibitors for treating cancer
发明人:BENNETT MICHAEL JOHN; ZEHNDER LUKE RAYMOND; NINKOVIC SACHA; KUNG PEI-PEI; MENG JERRY JIALUN; HUANG BUWEN
权利人:PFIZER
摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.