Stannylated allyl carbonates as versatile building blocks for the diversity oriented synthesis of allylic amines and amides
作者:Christian Bukovec、Uli Kazmaier
DOI:10.1039/c0ob00945h
日期:——
Stannylated allylic carbonates are suitable substrates for Pd-catalyzed allylic aminations. In DMF and with [allylPdCl]2 as catalyst the stannylated allyl amines formed can be directly coupled with electrophiles according to the Stille protocol, giving rise to highly functionalized buiding blocks in excellent yields.
Copper-Catalyzed Decarboxylative Functionalization of Conjugated β,γ-Unsaturated Carboxylic Acids
作者:Wei Zhang、Chengming Wang、Qiu Wang
DOI:10.1021/acscatal.0c03621
日期:2020.11.20
Copper-catalyzed decarboxylative coupling reactions of conjugated β,γ-unsaturated carboxylic acids have been achieved for allylic amination, alkylation, sulfonylation, and phosphinoylation. This approach was effective for a broad scope of amino, alkyl, sulfonyl, and phosphinoyl radical precursors as well as various conjugated β,γ-unsaturated carboxylic acids. These reactions also feature high regioselectivity
Anti-Markovnikov rearrangement in sulfur mediated allylic C–H amination of olefins
作者:Zhong Zhang、Hongguang Du、Jiaxi Xu、Pingfan Li
DOI:10.1039/c6cc05128f
日期:——
Hitherto unknown chemistry involving anti-Markovnikov rearrangement from secondary carbocations toward primary carbocations or primary triflates was discovered.
迄今尚未发现涉及从次级碳正离子向初级碳正离子或初级三氟甲磺酸酯的反马尔科夫尼科夫重排的未知化学。
[EN] HETEROCYCLIC COMPOUNDS AND THEIR USES<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEURS UTILISATIONS
申请人:AMGEN INC
公开号:WO2014152236A1
公开(公告)日:2014-09-25
Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.
提供了奥米卡替夫美卡比尔的某些药物配方以及其制备和使用方法。
Process for producing an oral sustained-release preparation of fasudil hydrochloride
申请人:ASAHI KASEI PHARMA CORPORATION
公开号:US20040131679A1
公开(公告)日:2004-07-08
Disclosed is an oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof, the preparation comprising at least one sustained-release coated particle comprising a core having a surface and a coating formed on the surface of the core, wherein the core contains the active ingredient and the coating comprises a coating base material and a specific insoluble auxiliary material, and wherein the preparation exhibits, with respect to the active ingredient, a specific dissolution rate, as measured by the dissolution test. By using the oral sustained-release preparation of the present invention, it becomes possible to surely control the release of fasudil hydrochloride from the preparation, so that the effect of the active ingredient is maintained for a long period of time. Therefore, the burden of the patient who has to take the preparation can be decreased and the compliance with respect to the administration of the preparation can be improved. Also disclosed is a method for evaluating an oral sustained-release preparation containing the active ingredient, wherein the evaluation is conducted with respect to the sustained-release ability of the active ingredient.