专利号:US-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
专利号:US-9493497-B2 优先权日:2012-04-26 标题:Carbamate glycolipid and use thereof 发明人:TASHIRO TAKUYA; MORI KENJI; SHIOZAKI MASAO; TANIGUCHI MASARU; WATARAI HIROSHI 权利人:RIKEN 摘要:The invention provides a compound effective as an antitumor active agent or vaccine adjuvant and an intermediate useful for the synthesis of the compound, as well as production methods thereof, and a medicament containing the novel compound. The compound is a carbamate glycolipid represented by the formula (I) n nwherein each symbol is as defined herein. The invention also provides a dendritic cell pulsed with the glycolipid.
专利号:US-2020369670-A1 优先权日:2019-05-09 标 题:REGIO-SELECTIVE SYNTHESIS OF IMIDAZO[1,2-a]PYRIMIDINES
专利号:CN-114423763-A 优先权日:2019-05-09 标 题 :Regioselective synthesis of imidazo[1,2-a]pyrimidines
专利号:EP-3966216-A1 优先权日:2019-05-09 标 题:Regio-selective synthesis of imidazo[1,2-a]pyrimidines
专利号:AU-2010100311-A4 优先权日:2009-11-12 标题:A process for the synthesis of polyhalogenated perhaloalkylaniline compounds