专利号:US-11485721-B2 优先权日:2017-11-21 标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses 发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN 权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST 摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.
参考标题:Metal-Free Synthesis Of Pharmaceutically Important Biaryls By Photosplicing 作者:Florian Kloss,Toni Neuwirth,Veit G. Haensch,Christian Hertweck |发布日期:2018.10.26 摘要:Neuroprotective And Cholesterol‐lowering Agents As Well As Antiarthritic Non‐steroidal Antiinflammatory Drugs (Nsaids). The New Method Was Successfully Employed In A Total Synthesis Of Cannabinol, An Important Analgesic And Antiemetic Therapeutic. We Also Report A Metal‐free Synthesis Of Key Building Blocks Used For The Preparation Of Sartans, Antihypertensive Agents That Rank Among The Top Blockbuster