(R)-1-Benzyloxy-N-Tert-Butoxycarbonyl-2-Propylamine置于palladium Dihydroxide Ruthenium Trichloride,Sodium Periodate,氢气体系中,用 甲醇,四氯化碳,水,乙腈 作为反应溶剂,化学反应 5.0H,反应生成 Boc-D-丙氨酸 参考文献:Synthesis Of Chiral α-Amino Acids 标题:Synthesis Of Chiral α-Amino Acids 摘要:A Novel Method For The Synthesis Of Chiral Alpha-Amino Acids Has Been Developed Where The Acid Functionality Was Constructed By Oxidizing A Hydroxymethyl Group Introduced By Evans' Method In The Alpha-Position Of An Appropriate Acid Substrate And The Amino Part Came From The Amide Of The Original Carboxyl Group Following A Modified Hofmann Rearrangement Reaction. (C) 2002 Published By Elsevier Science Ltd. DOI:10.1016/s0040-4039(02)02433-4
专利号:WO-2023030277-A1 优先权日:2021-08-30 标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD 摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.
专利号:US-5026773-A 优先权日:1987-03-11 标 题 :Apparatus for a solid phase synthesis of peptide analogs 发明人:STEEL SAMUEL 权利人:STEEL SAMUEL 摘要:A novel polymeric disc, wafer or similarly shaped resin for carrying out the synthesis of peptide analogs via solid phase peptide synthesis techniques is provided. The polymeric disc or wafer of the invention may be made out of those resin materials presently used in bead form in solid phase peptide synthesis, such as, benzhydrylamine resins, Boc-aminoacyl-4-(oxymethyl)-phenyacetamidomethyl (Pam) resin, polyamide resins and chloromethyl resins. The disc or wafer of the invention should, preferably, have a thickness of 200-400 mu m and may be of any suitable length or width. A process for the synthesis of peptide analogs utilizing the polymeric disc or wafer of the present invention is also disclosed.
专利号:US-4396542-A 优先权日:1980-02-14 标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production 发明人:WENGER ROLAND 权利人:SANDOZ LTD 摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.
专利号:US-5212288-A 优先权日:1990-02-20 标 题:Temporary minimal protection synthesis of serine-containing polypeptides 发明人:NESTOR JR JOHN J; MCCLURE NATALIE L; ARZENO HUMBERTO 权利人:SYNTEX INC 摘要:In a process for the solid phase synthesis of a polypeptide containing at least one serine residue, the improvement comprising temporarily protecting the side chain of the serine residue with a protecting group which is removed immediately following the addition of the serine to the peptide chain.
专利号:US-4554351-A 优先权日:1980-02-14 标 题:Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production 发明人:WENGER ROLAND 权利人:SANDOZ LTD 摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.
专利号:US-2017320908-A1 优先权日:2014-11-19 标题 :Solid phase synthesis of cyclic amino acid molecules 发明人:HICKEY JENNIFER L; MANCUSO JOHN; MARSAULT ERIC; ROUGHTON ANDREW L; TREDER ADAM P; TREMBLEY MARIE-CLAUDE J; YUDIN ANDREI K; ZARETSKY SERGE 权利人:ENCYCLE THERAPEUTICS; GOVERNING COUNCIL OF THE UNIV OF TORONTO; UNIV SHERBROOKE 摘要:The present invention relates to cyclic amino acid molecules and methods of preparing the same, and in particular the macrocyclization of amino acids or linear peptides bound to a solid support.
参考标题: An Improved Process For The Preparation Of Lacosamide Procédé Amélioré De Préparation De Lacosamide 摘要:The Present Invention Relates To An Improved Process For The Synthesis Of (R)- Lacosamide In Which Free Base Of O-Methyl-N-Benzyl-D-Serinamide Is Not Isolated Before Acylation. The Process Avoids The Use Of Column Chromatography And Chiral Resolution For The Preparation Of Different Stages Of Lacosamide.
合成参考文献
摘要:Ramesh, S.; Cherkupally, P.; Govender, T.; Kruger, H. G.; de la Torre, B. G.; Albericio, F., Science of Synthesis Knowledge Updates, (2017) 1, 371.