Treatment of GLC1A glaucoma with non-steroidal glucocorticoid antagonists
申请人:Alcon Laboratories, Inc.
公开号:US06051573A1
公开(公告)日:2000-04-18
Compositions of non-steroidal glucocorticoid antagonists for treating GLC1A glaucoma and methods for their use are disclosed.
非甾体糖皮质激素拮抗剂的组合物,用于治疗GLC1A型青光眼的方法已被披露。
Preparation of Nitrogen-Containing π-Deficient Heteroaromatic Grignard Reagents: Oxidative Magnesiation of Nitrogen-Containing π-Deficient Halogenoheteroaromatics Using Active Magnesium
作者:Osamu Sugimoto、Shigeru Yamada、Ken-ichi Tanji
DOI:10.1021/jo026492a
日期:2003.3.1
The oxidative magnesiation of nitrogen-containing pi-deficient halogenoheteroaromatics usingactive magnesium was accomplished. Both magnesiation followed by addition of a carbonyl compound (Grignard reaction) and magnesiation in the presence of a carbonyl compound (Barbier reaction) were carried out to afford the corresponding product. Especially, the latter method enabled fused halogenodiazines such
The Grignard reaction is one of the most common synthetic pathways in organic chemistry and has widely been used in the preparation of fine chemicals and pharmaceutical intermediates. The reaction's reproducibility can be affected by several factors (metal purity, degree of association in solution, Schlenk equilibrium) and its activation with chemical, mechanical, sonochemical or electromagnetic treatments
others. The scalable syntheses proceed in a few steps. The incorporation of AZARYPHOS ligands (L) into complexes [RuCp(L)2(MeCN)][PF6] (Cp=cyclopentadienyl) gives catalysts for the anti‐Markovnikov hydration of terminalalkynes of the highest known activities. Electronic and steric ligand effects modulate the reaction kinetics over a range of two orders of magnitude. These results highlight the importance
[1,2]-Anionic Rearrangement of 2-Benzyloxypyridine and Related Pyridyl Ethers
作者:Jingyue Yang、Gregory B. Dudley
DOI:10.1021/jo901707x
日期:2009.10.16
An anionic rearrangement of 2-benzyloxypyridine is described. Pyridine-directed metalation of the benzylic carbon leads to 1,2-migration of pyridine via a postulated associative mechanism (addition/elimination). Several aryl pyridylcarbinols were obtained in high yields. A formal synthesis of carbinoxamine, an antihistamine drug used for the treatment of seasonal allergies and hay fever, emerges from