专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:EP-1611083-B1 优先权日:2003-03-25 标 题:Synthesis of 2-chloromethyl-6-methylbenzoic acid esters 发明人:MAIER CLAUS-JUERGEN; METZENTHIN TOBIAS; GRAESER JOACHIM; BICKER RICHARD; MANERO JAVIER 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:The invention relates to a method for producing compounds of formula (I) wherein R represents H, optionally halogen-substituted alkyl, cycloalkyl or aryl, alkyl-aryl or heteroaryl, and at least one CH2 group can be replaced by O in alkyl and cycloalkyl. Said compounds of formula (I) are valuable intermediates in the synthesis of PPAR agonists.
专利号:US-6989462-B2 优先权日:2003-03-25 标题:Synthesis of 2-chloromethyl-6-methylbenzoic ester 发明人:MAIER CLAUS-JUERGEN; METZENTHIN TOBIAS; GRAESER JOACHIM; BICKER RICHARD; MANERO JAVIER 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:A process is described for preparing compounds of formula (I) n nwhere R is H, optionally halogen-substituted alkyl, cycloalkyl, aryl, alkyl-aryl or heteroaryl, and, in alkyl and cycloalkyl, one or more CH 2 groups may be replaced by —O—. The compounds of the formula (I) are valuable intermediates in the synthesis of PPAR agonists.
专利号:US-6528275-B1 优先权日:1996-04-24 标题:Substrates and inhibitors of proteolytic enzymes 发明人:QUIBELL MARTIN; JOHNSON TONY; HART TERANCE 权利人:MEDIVIR UK LTD 摘要:The present invention relates to the field of compounds which are substrates or inhibitors of proteolytic enzymes and to apparatus and methods for identifying substrates or inhibitors for proteolytic enzymes. We have devised a combinatorial method for the rapid indentification of binding motifs which will greatly expedite the synthesis of inhibitors of a variety of proteolytic enzymes such as aspartyl proteases, serine proteases, metallo proteases and cysteinyl proteases.
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:US-2005124683-A1 优先权日:2003-09-17 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:ALEGRIA LARRY A; CANAN-KOCH STACIE S; DRESS KLAUS R; HUANG BUWEN; KUMPF ROBERT A; LEWIS KATHLEEN K; MATTHEWS JEAN J; SAKATA SYLVIE K; VIRGIL SCOTT C 权利人:AGOURON PHARMA 摘要:The present invention relates to a series of chemical compounds useful as Human Immunodeficiency Virus (HIV) protease inhibitors and to the use of such compounds as antiviral agents. The invention further relates to pharmaceutical compositions containing such antiviral agents, and their uses and materials for their synthesis