Direct Vicinal Difunctionalization of Thiophenes Enabled by the Palladium/Norbornene Cooperative Catalysis
作者:Renhe Li、Yun Zhou、Xiaolong Xu、Guangbin Dong
DOI:10.1021/jacs.9b10857
日期:2019.12.4
thiophenes can be difunctionalized site- and regio-selectively at the C4 and C5 positions in good yields, enabled by an arsine ligand and a unique amide-based NBE. The synthetic utility has been shown in derivatizations of complex bioactive compounds and an open-flask gram-scale preparation. Preliminary results have been obtained in the difunctionalization of furans and a direct C4-selective arylation of
Redox‐Neutral Vicinal Difunctionalization of Five‐Membered Heteroarenes with Dual Electrophiles
作者:Renhe Li、Guangbin Dong
DOI:10.1002/anie.202110971
日期:2021.12.6
A new reaction mode of palladium/norbornene (Pd/NBE) cooperative catalysis is reported involving the selective coupling of two different carbon-based electrophiles for vicinal double C-H functionalization of five-membered heteroarenes in a site-selective and redox-neutral manner. The key is to use alkynyl bromides as the second electrophile, which allows vicinal difunctionalization of a wide range
Palladium-catalyzed direct alkynylation of thiophenes with halosilylacetylenes
作者:Hayate Kato、Naofumi Tsukada
DOI:10.1016/j.tetlet.2021.152869
日期:2021.3
Silylethynylthiophenes were obtained from palladium-catalyzedalkynylation of various thiophenes with 1-halo-2-silylacetylenes. The α-position of thiophenes was alkynylated with high regioselectivity. The terminal silyl groups of products could be replaced by several functional groups.
Benzo-fused lactams promote release of growth hormone
申请人:Merck & Co., Inc.
公开号:US05284841A1
公开(公告)日:1994-02-08
There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
The present invention provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Compounds of formula (I) are also provided.