专利号:US-2007293706-A1 优先权日:2004-11-01 标 题:Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones 发明人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 权利人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 摘要:1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.
专利号:WO-9000622-A1 优先权日:1988-07-08 标题 :Oligonucleotide hybridization probes and means for the synthesis of the most preferred probes 发明人:KWIATKOWSKI MAREK; SUND CHRISTIAN; HURSKAINEN PERTTI 权利人:WALLAC OY; PHARMACIA AB 摘要:Oligonucleotide probe labeled at one of its teminal positions with a non-linear branched polymer carrying a plurality of negatively charged groups, preferably phosphodiester groups, and optionally also analytically indicatable groups covalently linked to terminal ends of the branches of said polymer. The preferred indicatable groups are lanthanide chelates. A compound that can be used for the synthesis of the probe is also disclosed. The compound has formula (I), where R1 and R2 are lower alkyl; R3 is lower alkyl (C1-C7), or aryl each of which optionally being provided with electron-withdrawing substituents; and A1, A2 and A3 are hydrogen, A'-O-B, A''-O-B or A'''-O-B, at most one of A1-3 being hydrogen and A', A'' and A''' being a hydrocarbon chain providing a distance of 5-9 atoms between the phosphorous atom and the oxygen directly bound to B, and B being a protecting group. In the preferred compound at least two of A1-3 are identical while the other is hydrogen.
专利号:US-9975832-B2 优先权日:2014-12-29 标题:Process for the preparation of ospemifene and fispemifene 发明人:CRISTIANO TANIA; ALPEGIANI MARCO 权利人:OLON SPA 摘要:Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH 2 CH 2 —Y of formula 7, wherein X is a leaving group and Y is the —(OCH 2 CH 2 ) n OH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
专利号:US-2025129050-A1 优先权日:2022-01-26 标 题 :Synthesis of a kif18a inhibitor 发明人:CAILLE SEBASTIEN; GREENE DANIEL GERARD; CORBETT MICHAEL THOMAS; WEI CAROLYN 权利人:AMGEN INC 摘要:The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).
专利号:US-9220795-B2 优先权日:2011-09-22 标题 :Indole derivatives 发明人:WADSWORTH HARRY JOHN; O'SHEA DENNIS; PASSMORE JOANNA; TRIGG WILLIAM; EEWAN AMANDA; SHAN BO 权利人:GE HEALTHCARE LTD 摘要:An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
专利号:US-8790619-B2 优先权日:2009-03-27 标题 :Indole derivatives 发明人:WADSWORTH HARRY JOHN; SHAN BO; O'SHEA DENNIS; PASSMORE JOANNA MARIE; TRIGG WILLIAM JOHN; EWAN AMANDA 权利人:WADSWORTH HARRY JOHN; SHAN BO; O'SHEA DENNIS; PASSMORE JOANNA MARIE; TRIGG WILLIAM JOHN; EWAN AMANDA; GE HEALTHCARE LTD 摘要:An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
[参考文献]: Fodil Bouazza, Et Al. Total Synthesis And Conformational Analysis Of The Antifungal Agent (-)-Pf1163B. Org Lett. 2003 Oct 30;5(22):4049-52.
合成参考文献
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