专利号:US-9926291-B2 优先权日:2007-03-27 标 题 :Synthesis of thiohydantoins 发明人:OUERFELLI OUATHEK; DILHAS ANNA; YANG GUANGBIN; ZHAO HONG 权利人:SLOAN KETTERING INST CANCER RES 摘要:A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
专利号:US-2023046065-A1 优先权日:2019-11-25 标题 :MERGING C(sp3)-H ACTIVATION WITH DNA-ENCODING 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Palladium-catalyzed C(sp3)—H arylation of aliphatic carboxylic acids, amides and ketones with BNA-encoded aryl iodides in water is disclosed, Furthermore, sequential C—H arylation chemistry enabled the on-DNA synthesis of structurally-diverse scaffolds containing enriched C(sp3) character, chiral centers, cyclopropane, cyclobutane, and heterocycles. That new chemistry permits preparation of a DNA—encoded library (BEL) technology that can dramatically expedite hit identification in drug discovery owing to its ability to perform protein affinity selection with millions or billions of molecules in a single experiment. The sequential functionalization of multiple C—H bonds provides an unique avenue for creating diversity and complexity from simple starting materials. The use of water as solvent, the presence of DMA, and the extremely low concentration of DMA-encoded coupling partners (0.001 M) have previously hampered the development DMA-encoded C(sp3)—H activation reactions, but many of those hurdles have now been overcome.
专利号:WO-2008119015-A2 优先权日:2007-03-27 标 题 :Synthesis of thiohydantoins
专利号:US-8987452-B2 优先权日:2007-03-27 标 题:Synthesis of thiohydantoins
专利号:US-2010190991-A1 优先权日:2007-03-27 标题 :Synthesis of thiohydantoins
专利号:US-9512103-B2 优先权日:2007-03-27 标题:Synthesis of thiohydantoins