N-Boc-D-苯丙氨醇置于重铬酸吡啶体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成Boc-D-苯丙氨酸 参考文献:Versatile Routes To Chiral 4-Substituted 2-Oxazolidinones And .Alpha.-Amino Acids. Use Of Chiron,(4+2) Cycloadducts Of Dialkyl Azodicarboxylates And 2-Oxazolones. 标题:Versatile Routes To Chiral 4-Substituted 2-Oxazolidinones And .Alpha.-Amino Acids. Use Of Chiron,(4+2) Cycloadducts Of Dialkyl Azodicarboxylates And 2-Oxazolones. 摘要:3-[(1S)-2-烷氧基-1-阿波伞烷酮]-2-噁唑酮与二烷基偶氮二甲酸酯的热反应导致专一性形成[4+2]型环加成物,具有中等程度的非对映面选择性,这些产物作为多功能的手性合成前体,可用于合成多种4-烷基和4-芳基-2-噁唑啉酮以及α-氨基酸. Doi:10.1248/cpb.40.1077
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-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
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.
专利号:WO-2005087794-A1 优先权日:2004-03-12 标题:Process for octreotide synthesis 发明人:IAROV ALEXEI; AVRUTOV ILYA; LAZAROWYCH NATALIE; HOULDSWORTH STEPHEN 权利人:DALTON CHEMICAL LAB INC; IAROV ALEXEI; AVRUTOV ILYA; LAZAROWYCH NATALIE; HOULDSWORTH STEPHEN 摘要:A hybrid solid phase-liquid phase method of octreotide synthesis is described, along with methods for preparation of intermediate compounds useful in the synthesis of Octreotide. The method comprises liquid phase condensation of two or three peptide blocks, of which at least one is synthesized by solid-phase method. Each block contains two or more amino acid residues. The method combines the time and labor effectiveness of the solid-phase method with relative cheapness and easiness of purification of the product, characteristic of the liquid-phase method.
专利号:US-4794150-A 优先权日:1987-03-11 标题: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 synthsis 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 μm and may be of any suitable length or width. A process for the synthsis of peptide analogs utilizing the polymeric disc or wafer of the present invention is also disclosed.
专利号:US-9388212-B2 优先权日:2013-02-21 标 题:Solid phase peptide synthesis via side chain attachment 发明人:BARLOS KLEOMENIS K 权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A 摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.