专利号:US-10087221-B2 优先权日:2013-03-21 标题 :Synthesis of hydantoin containing peptide products 发明人:HENKEL BERND 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:The present invention relates to a method of synthesizing a peptide product comprising at least one hydantoin group. The peptide product may be used as a reference material for the quality control of pharmaceutical peptides, particularly for the quality control of exendin peptides. Further, the invention relates to hydantoin building blocks, a method for manufacturing such building blocks and their use for the synthesis of peptide products.
专利号:US-5880295-A 优先权日:1994-02-16 标 题 :Process for the preparation of diamine intermediates useful in the synthesis of HIV protease inhibitors 发明人:KALTENBACH III ROBERT FRANK 权利人:DU PONT PHARM CO 摘要:The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas. ##STR1##
专利号:US-6022977-A 优先权日:1997-03-26 标 题 :Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic acids 发明人:ZHANG LIN-HUA; ANZALONE LUIGI; PESTI JAAN A; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
专利号:US-5530124-A 优先权日:1994-06-30 标 题:Method for preparing cyclic ureas and their use for the synthesis of HIV protease inhibitors 发明人:RADESCA LILIAN A; HARRIS GREGORY D; WAT EDWARD K W; WALTERMIRE ROBERT E 权利人:DU PONT MERCK PHARMA 摘要:This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.
专利号:WO-2024146948-A1 优先权日:2023-01-05 标题:Peptide synthesis method involving sterically hindered tri-tert-butyl-tryptophan (tbt) residue 发明人:EKSTEEN JACOBUS JOHANNES; SVENDSEN JOHN SIGURD; MALMEDY FLORENCE; GUEVARA JONATHAN 权利人:AMICOAT AS 摘要:The invention is directed to a method of peptide synthesis comprising reacting a compound of Formula (I) or a salt thereof with a carbodiimide reagent to form an O-acylisourea intermediate; reacting the O-acylisourea intermediate with an additive to form an activated ester; and reacting the activated ester with an amino-containing moiety which is an amino acid, a peptide or a salt thereof comprising an amino group, wherein the amino group forms an amide bond with the carbonyl marked * in Formula (I); wherein the compound of Formula (I) has the structure: and wherein R1 and R2 are as defined in the disclosure. The invention is also directed to a compound of Formula (III) as defined in the disclosure or a salt thereof.
专利号:WO-0043352-A1 优先权日:1999-01-22 标题:A method for the synthesis of compounds of formula 1 and derivatives thereof
参考文献:10.1111/j.1399-3011.2005.00312.x 摘要:Haynes SR, Hagins SD, Juban MM, Elzer PH, Hammer RP. Improved solid-phase synthesis of alpha,alpha-dialkylated amino acid-rich peptides with antimicrobial activity. J Pept Res. 2005 Dec;66(6):333–47. doi: 10.1111/j.1399-3011.2005.00312.x. 参考文献:10.1021/jm901788j 摘要:McHardy T, Caldwell JJ, Cheung K, Hunter LJ, Taylor K, Rowlands M, Ruddle R, Henley A, de Haven Brandon A, Valenti M, Davies TG, Fazal L, Seavers L, Raynaud FI, Eccles SA, Aherne GW, Garrett MD, Collins I. Discovery of 4-Amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides As Selective, Orally Active Inhibitors of Protein Kinase B (Akt). J. Med. Chem. 2010 Feb 12;53(5):2239–49. doi: 10.1021/jm901788j.