在 水体系中,化学反应生成帕莫酸 参考文献:Participation Of Two Carboxyl Groups In Phosphodiester Hydrolysis. 2. A Kinetic,Isotopic,And 31P NMR Study Of The Hydrolysis Of A Phosphodiester With Carboxyl Groups Fixed In An Attack Conformation 标题:Participation Of Two Carboxyl Groups In Phosphodiester Hydrolysis. 2. A Kinetic,Isotopic,And 31P NMR Study Of The Hydrolysis Of A Phosphodiester With Carboxyl Groups Fixed In An Attack Conformation 摘要:The Phosphodiesters Of 4,4'-Methylenebis(3-Hydroxy-2-Naphthoic Acid) (4) And 3-Carboxy-2,2'-Dihydroxy-Diphenylmethane (5) Are Constrained Into A Cyclic Structure Such That The Oxygens Of The Two O-Carboxy Groups Of 4 And The Single O-Carboxy Group Of 5 Have Restricted Stereospecific Positions With An O-Co2-Oxygen To Phosphorus Distance Of 3.7 Angstrom. In The Hydrolysis Of 4,P-31 NMR And HPLC Data Show The Existence Of An Intermediate Cyclic Acyl Phosphate In The G,G Conformation. The O-18 Isotopic Effects On P-31 Chemical Shifts Show Incorporation Of Two O-18 Atoms In The Product H3Po4. This Observation Is Consistent With Intramolecular O-Co2-Nucleophilic Attack On Phosphorus To Provide An Acyl Phosphate Intermediate Which Undergoes Hydrolytic Cleavage By Ho-/(Ho-)-O-18 Attack On Phosphorus (One O-18 Incorporation) To Provide A Phosphate Monoester Which Also Undergoes Hydrolysis With A Second O-18 Incorporation On Phosphorus. For Hydrolysis Of 4,The Ph Vs Log K(Obsd) Profile,The Values Of The Deuterium Solvent Kinetic Isotope Effect,And The Activation Entropy Accord A Mechanism Which Involves Intramolecular Attack Of O-Co2-On The Phosphate Phosphorus Assisted By The O-Co2H As A General Acid Catalyst,The Latter Can Involve O-Co2H Hydrogen Bonding To The-(Po2-)-Oxygen(S) And/or Leaving Phenolic Oxygen. At Neutrality,4 Hydrolyzes Ca. 10(4) Fold Faster Than 5 Which Only Has One O-Carboxy Group And 10(8)-10(9)-Fold Faster Than Diphenyl Phosphate. Doi:10.1021/ja00154A006
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-9643915-B2 优先权日:2013-03-15 标题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-9708354-B2 优先权日:2013-03-15 标 题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:EP-0443532-B1 优先权日:1990-02-20 标题:Temporary minimal protection synthesis of LH-RH analogs 发明人:NESTOR JOHN J JR; MCCLURE NATALIE L 权利人:SYNTEX INC 摘要:A solid phase synthesis of LH-RH analogs in which the amino acids serine and histidine, if present, are side chain protected during the synthesis with groups labile to selected alpha -amino or deprotecting agents.
专利号:WO-2004011474-A1 优先权日:2002-07-31 标题:Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
1: Park EJ, Amatya S, Kim MS, Park JH, Seol E, Lee H, Shin YH, Na DH. Long-acting injectable formulations of antipsychotic drugs for the treatment of schizophrenia. Arch Pharm Res. 2013 Jun;36(6):651-9. doi: 10.1007/s12272-013-0105-7. Epub 2013 Apr 1. Review. doi: 10.1016/B978-0-12-398314-5.00002-7. Review. doi: 10.1124/mol.110.067645. Epub 2010 Jul 22. Review. doi: 10.1016/j.ymeth.2009.03.022. Epub 2009 Apr 9. Review.
合成参考文献
参考文献:10.1107/s1600536806005812 摘要:Haynes DA, Van de Streek J, Burley JC, Jones W, Motherwell WDS. Pamoic acid determined from powder diffraction data. Acta Crystallogr E Struct Rep Online. 2006 Feb 28;62(3):o1170–2. doi: 10.1107/s1600536806005812. 参考文献:10.1016/j.poly.2009.07.050 摘要:Baghel GS, Rao CP. Pamoic acid in forming metallo-organic framework: Synthesis, characterization and first crystal structure of a dimeric Ti(IV) complex. Polyhedron. 2009 Nov;28(16):3507–14. doi: 10.1016/j.poly.2009.07.050.