📜三氟乙腈,三氟乙酸 反应生成 双三氟乙酰胺 参考文献:Fluorocarbon Nitrogen Compounds. Vii.1 The Indirect Fluorination Of Some Fluorocarbon Nitrogen Derivatives2 标题:Fluorocarbon Nitrogen Compounds. Vii.1 The Indirect Fluorination Of Some Fluorocarbon Nitrogen Derivatives2 摘要:The Indirect Fluorination Of Some Fluorocarbon Nitrogen Compounds Has Been Investigated And Reactions Of The Following Functional Groups Have Been Determined Under Mild Conditions:-N=c<,N C-,C-(-N = C<)(8),>N-H,>Ncof,-N = C = O,-Nhcof,-Conh2 And-Conhco-. Fluorocarbon N-F Compounds Can Be Synthesized In Certain Cases By The Action Of Silver Difluoride On Carbon-Nitrogen Unsaturation,By Replacement Of Amine Hydrogen Or By Cleavage Of An Acyl Group From Nitrogen. Rearrangement And Coupling Of The Free Radical Intermediates Are Competitive With N-F Bond Formation,Coupling Becoming More Important With Progressively Milder Conditions. Volatile Fluorocarbon Isocyanates Can Be Conveniently Prepared From The Corresponding Amides By Reaction With Agf2,And Fluorocarbon Azoalkanes,Rfcf2N = Ncf2Rf,From Nitriles By Use Of The Same Reagent. Similarity Of The Isocyanate Synthesis To The Hofman And Curtius Reactions Is Discussed. DOI:10.1021/ja01502A027
专利号:WO-2013132505-A1 优先权日:2012-03-09 标题 :Improved process for preparation of octreotide by solution phase peptide synthesis 发明人:KOTA SATYANARAYANA; TALLAPANENI VENKATESWARLU; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD; KOTA SATYANARAYANA; TALLAPANENI VENKATESWARLU; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 摘要:The present invention relates to a novel processes for commercial production of pharmaceutical grade octreotide using classical solution phase peptide synthesis in high yield and purity and using inexpensive amino acid derivatives. Thus the protected octapeptide alcohol Boc -D- Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - Cys (Trt) - Thr - OL is prepared by condensation of hexapeptide acid Boc -D - Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - OH with dipeptide alcohol H- Cys (Trt) - Thr - OL. The hexapeptide Boc -D- Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - OMe is prepared by condensing Boc - D - Phe - Cys (Trt) - OH with tetrapeptide H-Phe -D - Trp - Lys (Boc) - Thr - OMe followed by hydrolysis. The linear octapeptide alcohol is treated with cocktail mixture TFA /water/ TIS (9.0:0.5:0.25), in one step removes the Trt and Boc groups, followed by oxidation with hydrogen peroxide to affords octreotide.
专利号:CN-102686601-A 优先权日:2009-11-16 标 题 :Synthesis of Ac-Arg-cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2
专利号:WO-2011060355-A1 优先权日:2009-11-16 标题 :Process for the synthesis of ac-arg-cyclo(cys-d-ala-his-d-phe-arg-trp-cys)-nh2
专利号:JP-2013510881-A 优先权日:2009-11-16 标题 :Method for the synthesis of Ac-Arg-cyclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys) -NH2
参考标题:Blue Light-Promoted N-H Insertion Of Amides, Isatins, Sulfonamides And Imides Into Aryldiazoacetates: Synthesis Of Unnatural α-Aryl Amino Acid Derivatives 作者:Celso Y. Okada,Caio Y. Dos Santos,Igor D. Jurberg |发布日期:2020.12 摘要:A Photochemical Protocol Using Blue Light Allows The N-H Insertion Of Amides, Isatins, Sulfonamides And Imides Into Aryldiazoacetates To Afford The Corresponding α-Amino Esters. This Method Is Experimentally Simple, Inexpensive And Tolerates Numerous Functional Groups, Thus Allowing The Straightforward Preparation Of A Variety Of α-Aryl Amino Acid Derivatives In Good Yields.
合成参考文献
参考文献:10.1016/s0277-5387(99)00055-8 摘要:Narula PM, Day CS, Powers BA, Odian MA, Lachgar A, Pennington WT, Noftle RE. Characterization and crystal structures of some fluorinated imides. Polyhedron. 1999 Apr;18(12):1751–9. doi: 10.1016/s0277-5387(99)00055-8.