Transition-Metal-Free Synthesis of Oxindoles by Potassium tert-Butoxide-Promoted Intramolecular α-Arylation
摘要:
Potassium tert-butoxide-mediated intramolecular alpha-arylations of fluoro- and chloro-substituted anilides provide oxindoles in DMF at 80 degrees C. In this manner, diversely substituted products have been obtained in moderate to high yields.
Transition-Metal-Free Synthesis of Oxindoles by Potassium tert-Butoxide-Promoted Intramolecular α-Arylation
摘要:
Potassium tert-butoxide-mediated intramolecular alpha-arylations of fluoro- and chloro-substituted anilides provide oxindoles in DMF at 80 degrees C. In this manner, diversely substituted products have been obtained in moderate to high yields.
Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
DIHYDRONAPHTHYRIDINYL AND RELATED COMPOUNDS FOR USE IN TREATING OPHTHALMOLOGICAL DISORDERS
申请人:Jones Simon
公开号:US20100286136A1
公开(公告)日:2010-11-11
The invention provides methods of using dihydronaphthyridinyl and related compounds to treat opthalmological disorders, such as, wet age-related macular degeneration, diabetic retinopathy, and high myopia. Pharmaceutical compositions and methods of synthesizing the dihydronaphthyridinyl and related compounds are provided.
to the efficient and convenient synthesis of amides as their great application in medicinal chemistry. However, some problems still exist in the preparation of amides, such as atom-economic. Here, a new and efficient method to prepare amides by the carbonylation of amines was developed without CO gas and palladium catalyst. Mo(CO)6 was employed as carbonyl source, different amines could tolerate the
酰胺类化合物在药物化学中的广泛应用对高效便捷地合成酰胺类具有重要意义。然而,酰胺的制备仍存在原子经济等问题。在这里,开发了一种在没有 CO 气体和钯催化剂的情况下通过胺的羰基化制备酰胺的新有效方法。采用Mo(CO) 6作为羰基源,不同的胺可以耐受反应条件,并以良好至优异的收率得到相应的酰胺。提出了一种可能的反应机理。该方法为酰胺的合成提供了一种潜在的途径。