[EN] PROCESSES AND INTERMEDIATES FOR THE PRODUCTION OF FULVESTRANT<br/>[FR] PROCÉDÉS ET INTERMÉDIAIRES DESTINÉS À LA PRODUCTION DE FULVESTRANT
申请人:SYNTHON BV
公开号:WO2010043404A1
公开(公告)日:2010-04-22
The invention relates to a compound of formula (1) wherein R1 represents hydrogen or an acetyl group and R2 represents a methyl, acetyl, or benzyl group, to its preparation, and to its use in the preparation of fulvestrant.
[EN] COMPOUNDS THAT INHIBIT MCL-1 PROTEIN<br/>[FR] COMPOSÉS INHIBANT LA PROTÉINE MCL-1
申请人:AMGEN INC
公开号:WO2018183418A1
公开(公告)日:2018-10-04
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (I), or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
[EN] TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE<br/>[FR] INHIBITEURS TRICYCLIQUES DE POLY(ADP-RIBOSE)POLYMÉRASE
申请人:NEWGEN THERAPEUTICS INC
公开号:WO2012166983A1
公开(公告)日:2012-12-06
The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-l(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP- ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.
Photoinduced Cross-Coupling of Aryl Iodides with Alkenes
作者:Yuliang Liu、Haoyu Li、Shunsuke Chiba
DOI:10.1021/acs.orglett.0c03935
日期:2021.1.15
A protocol for photoinduced cross-coupling of aryliodides having polar π-functional groups or elongated π-conjugation with alkenes has been developed. The radical cascade mechanism involving generation of aryl radicals via C–I bond homolysis of photoexcited aryliodides and their subsequent addition to alkenes is proposed. The method enables iodide-selective cross-coupling over other halogen leaving
Coordination-Induced Stereocontrol over Carbocations: Asymmetric Reductive Deoxygenation of Racemic Tertiary Alcohols
作者:Mayuko Isomura、David A. Petrone、Erick M. Carreira
DOI:10.1021/jacs.9b00862
日期:2019.3.20
intermediate tertiary carbocations. This approach has been implemented to achieve the first example of enantioselective reductive deoxygenation of tertiaryalcohols. This reduction occurs with high enantio- (up to 96% ee) and regioselectivity (up to >50:1 rr) by applying a novel Hantzsch ester analogue as a convenient hydride source. In-depth mechanistic studies support the involvement of a tertiary carbocation