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:WO-2024137329-A1 优先权日:2022-12-20 标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:WO-2024019698-A1 优先权日:2022-07-18 标题 :Photocatalytic synthesis of alpha, beta unsaturated carbonyl compounds and their intermediates 发明人:SUGURI TAKUYA; MARUYAMA YOUICHIROU; LIM CHERN-HOOI; QIAN GANG; LIU YUE; COPE ELANA 权利人:JSR CORP; NEW IRIDIUM INC 摘要:Described herein is a process of producing α,β unsaturated acids and amides and their intermediates via a photocatalytic reaction in the presence of a photocatalyst, oxygen, and optionally a solvent. The photocatalyst contains a tungstic acid or a salt of a tungstic acid. The process is simple, clean, and energy efficient, and provides good conversion, good selectivity, good turnover, and easy purification of end products.
专利号:US-2018312534-A1 优先权日:2015-10-16 标题:Fluorescent anticancer platinum drugs 发明人:SARKAR ARINDAM; MANDAL SWADHIN KUMAR; SENGUPTA ANIRUDDHA; BISWAS GOUTAM; DUTTA PRADIP; SHARMA RUPALI; RAJ JUSTIN PAUL; SURYAVANSHI HEMANT; KUMARI SMITA 权利人:INVICTUS ONCOLOGY PVT LTD 摘要:The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to fluorescent platinum based compounds. The disclosure further relates to synthesis of said fluorescent platinum based compounds, nanoparticles and compositions comprising said fluorescent platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by the fluorescence changes between aforesaid platinum based compounds and corresponding free ligands, nanoparticles and compositions.
专利号:US-2017233877-A9 优先权日:2011-06-17 标 题 :Synthesis of hetero compounds using dialkylcarbonate quaternation
专利号:US-10000487-B2 优先权日:2015-11-20 标 题 :Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers 发明人:SPRENGELER PAUL A; REICH SEIGFRIED H; WEBBER STEPHEN E; ERNST JUSTIN T 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. n nFor Formula IA and Formula IB compounds A 1 , A 2 , A 3 , A 4 , W 1 , W 2 , Y, X, R 1 , R 2 , R 3 , R 4a , R 4b , R 5a , R 5b , R 6 , R 7 , R 8 , R 9 , R 9a , R 9b , R 10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.