Synthesis of <i>N</i>-Glycosyl-2-oxindoles by Pd-Catalyzed N-Arylation of 1-Amidosugars
作者:Boris Letribot、Wafa Redjdal、Belkacem Benmerad、Franck Le Bideau、Mouâd Alami、Samir Messaoudi
DOI:10.1021/acs.orglett.0c01262
日期:2020.6.5
An efficient intramolecular Pd-catalyzed N-arylation of o-iodo-amidosugars for the synthesis of N-glycosylated oxindoles has been reported. The coupling reaction takes place in toluene and involves Pd(OAc)2/RuPhos catalyticsystems in the presence of K2CO3. This versatile approach was extended successfully to the synthesis of other N-glycosylated heterocycles.
已经报道了用于合成N-糖基化的羟吲哚的有效的分子内Pd催化的O-碘-氨基糖的N-芳基化。偶联反应在甲苯中进行,并且涉及在K 2 CO 3存在下的Pd(OAc)2 / RuPhos催化体系。这种通用方法已成功扩展到其他N-糖基化杂环的合成。
Aralykyl (arylethynyl)aralkyl amines and their use as vasodilators and
申请人:McNeilab, Inc.
公开号:US04661635A1
公开(公告)日:1987-04-28
Acetylenes of the formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2 q, Alk, R.sup.3, n and R.sup.4 are as defined herein and Ar.sup.1 and Ar.sup.2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.
Synthesis of 2-Phenylnaphthalenes through Gold-Catalyzed Dimerization via a Highly Selective Carbon Nucleophile Pathway
作者:Sinan Wang、Lei Zhang、Xiao Ding、Yu Zhou、Jinfang Wang、Hualiang Jiang、Hong Liu
DOI:10.1021/jo200352j
日期:2011.6.3
A protocol for the facile synthesis of 2-phenylnaphthalene has been developed. The benzyl carbon acts as a nucleophilic center in the presence of the amide nitrogen and acetate oxygen, affording the selective formation of a naphthalene scaffold through the dimerization of the reactants.
Acetylene amines and their use as vasodilators and antihypertensives
申请人:McNeilab, Inc.
公开号:US04725602A1
公开(公告)日:1988-02-16
Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.
Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.