专利号:US-9708317-B2 优先权日:2013-11-25 标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives 发明人:ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY 权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL 摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
专利号:US-8779207-B2 优先权日:2012-08-31 标题 :Method for synthesis of [6,6]-phenyl-C61-butyric acid methyl ester (PCBM) and fullerene derivatives 发明人:NG KA MING; ZHUANG JIANLE; TSENG NAI WEN; YU YONG 权利人:NG KA MING; ZHUANG JIANLE; TSENG NAI WEN; YU YONG; NANO & ADVANCED MATERIALS INST LTD 摘要:The present subject matter relates to methods for the synthesis of [6,6]-phenyl-C 61 -butyric acid methyl ester (PCBM) and fullerene derivatives in a yield of at least 40%.
专利号:US-12180182-B2 优先权日:2021-12-01 标题 :(Di)amination of activated allene compounds, derivatives thereof, and methods for synthesis of the same 发明人:DAI MINGJI 权利人:PURDUE RESEARCH FOUNDATION 摘要:One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.
专利号:US-2009162290-A1 优先权日:2005-09-09 标 题 :Method for the synthesis of penta-pendant enantiomer-pure chelators and process for therapeutically active bioconjugates preparation by a covalent binding thereof 发明人:BENES IVAN; CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R 1 , R 2 , R 3 , R 4 are groups forming an adequate enantiomer of the chelator; and X 1 -X 5 , Y 1 -Y 5 , Z 1 -Z 5 each individually forming pendant chelating groups.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:US-RE41614-E 优先权日:1998-09-30 标题 :Synthetic analogs of ecteinascidin-743 发明人:COREY ELIAS J 权利人:HARVARD COLLEGE 摘要:The present invention is directed to the synthesis and characterization of compounds having the formula: n n wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO 2 R′, NO 2 , NH 2 , NHR′, N(R′) 2 , NHC(â•?O)R′ NHC( â•?O ) R′ , CN, halogen, â•?O, C(â•?O)H, C(â•?O)R′, CO 2 H, CO 2 R′, C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH 2 , NO 2 , SH, CN, halogen, â•?O, C(â•?O)H, C(â•?O)CH 3 , CO 2 H, CO 2 CH 3 , C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R 7 and R 8 may be are joined into a carbocyclic or heterocyclic ring system; and wherein X 1 and X 2 are each independently defined as above for R 1 -R 8 R 1 - R 6 and R 9 , an each further includes specific preferred groups as defined herein.
[参考文献]: Hao Sun, Et Al. Highly Regio- And Stereoselective Synthesis Of Alpha-(N-Alkyl-N-P-Toluenesulfonyl)-Beta-Bromo-Ketones Via Ni(Oac)2-Catalyzed Aminobromination Of Chalcones. Chem Biol Drug Des. 2010 Mar;75(3):269-76.
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