N-Boc-L-Norvaline Ethyl Ester置于盐酸,水体系中,用 1,4-二氧六环 作为反应溶剂,化学反应生成 L-正缬氨酸乙酯盐酸盐 参考文献:Cyclic Phosphoramidates As Prodrugs Of 2'-C-Methylcytidine 标题:Cyclic Phosphoramidates As Prodrugs Of 2'-C-Methylcytidine 摘要:The Currently Approved Treatment For Hepatitis C Virus Infections Is A Combination Of Ribavirin And Pegylated Interferon. It Leads To A Sustained Virologic Response In Approximately Only Half Of The Patients Treated. For This Reason There Is An Urgent Need Of New Therapeutic Agents. 2'-C-Methylcytidine Is The First Nucleoside Inhibitor Of The Hcv Ns5B Polymerase That Was Efficacious In Reducing The Viral Load In Patients Infected With Hcv. The Application Of A Monophosphate Prodrug Approach Based On Unprecedented Cyclic Phosphoramidates Is Reported. Our Sar Studies Led To Compounds That Are Efficiently Converted To The Active Triphosphate In Human Hepatocytes. (C) 2009 Elsevier Masson Sas. All Rights Reserved. DOI:10.1016/j.Ejmech.2009.04.043
专利号:US-4902817-A 优先权日:1987-09-17 标 题 :Process for the synthesis of alpha n alkylated amino acids and esters thereof, application to the synthesis of carboxyalkyl dipeptides 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Stereoselective process for the industrial synthesis of compounds of formula (I): ##STR1## where R 1 is linear or branched lower alkyl with 1 to 6 carbon atoms, n R 2 is a linear or branched lower alkyl with 1 to 4 carbon atoms, n employing inexpensive starting materials and obtaining optimum yields. n Application to the synthesis of carboxyalkyl dipeptides.
专利号:US-4914214-A 优先权日:1987-09-17 标 题:Process for the industrial synthesis of perindopril 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Process for the industrial synthesis of perindopril, in which (2S,3aS,7aS)-2-carboxyperhydroindole is condensed with N-[(S)-1-carbethoxybutyl]-(S)-alanine after protection of the carboxyl group, the product resulting from the condensation being then subjected to deprotection of the carboxyl carried by the heterocyclic ring. n The (2S,3aS,7aS)-2-carboxyperhydroindole and N-[(S)-1-carbethoxybutyl]-(S)-alanine are themselves obtained in excellent conditions from 2-carboxyindole and from L-alanine respectively, both available on an industrial scale.
专利号:EP-0308340-B1 优先权日:1987-09-17 标 题 :Process for the synthesis of n-alkylated alpha-amino acids and their esters, use in the synthesis of carboxyalkyl dipeptides
专利号:AU-606992-B2 优先权日:1987-09-17 标题:Process for the synthesis of alpha n alkylated amino acids and esters thereof. application to the synthesis of carboxyalkyl dipeptides.
专利号:IE-60994-B1 优先权日:1987-09-17 标题 :Process for the synthesis of alpha N alkylated amino acids and esters thereof. Application to the synthesis of carboxyalkyl dipeptides
专利号:EP-0308341-B1 优先权日:1987-09-17 标 题 :Process for the industrial synthesis of perindopril and for its principal synthesis intermediates
参考标题:A [3+3] Cyclization Strategy For Asymmetric Synthesis Of Alkyl Substituted Piperidine-2-Ones Using 1,2-Cyclic Sulfamidates: A Formal Synthesis Of (S)-Coniine From L-Norvaline 作者:Abdullah Karanfil,Berrin Balta,Mustafa Eskici |发布日期:2012.12 摘要:β-Unsaturated Esters After Acidic Hydrolysis. Hydrogenation Of The Unsaturated Esters And Subsequent Thermal Cyclization Afforded The Related Alkyl Substituted Piperidine-2-Ones. This Approach Represents A Novel [3+3] Cyclization Strategy For The Asymmetric Synthesis Of Alkyl Substituted Piperidin-2-Ones. Efficiency Of The Cyclization Process Is Illustrated By A Formal Asymmetric Synthesis Of (S)-Coniine From L-Norvaline