专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:WO-2011024039-A1 优先权日:2009-08-25 标题 :Synthesis of novel 5-(2-(phenylsulfonyl)ethyl)-1h-indole derivatives 发明人:POTLURI RAMESH BABU; KODALI HARI PRASAD; VENTURI SRINIVASA RAO; TADIMALLA VENKATA SRIHARI 权利人:POTLURI RAMESH BABU; KODALI HARI PRASAD; VENTURI SRINIVASA RAO; TADIMALLA VENKATA SRIHARI 摘要:An objective of the present invention is to develop commercially viable methods for the synthesis of 5-[2-phenylsulfony)ethyl]-1H-indole of Formule (II), where R 1 and R 2 are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (II). Another objective of the present invention is to convert the product Formula (II) to Formula (I) in high yields, where R 1 and R 2 are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (I). One of the first processes attempted was by reacting the indole derivative of Formula (III) with aryl vinyl sulphones of Formula (V) as shown in Scheme-III. Another process attempted was by reacting the aniline derivative of Formula (VI) with aryl sulphones of Formula (VII) as shown in Scheme-III. Scheme IV.
专利号:US-10865163-B2 优先权日:2017-12-20 标题:Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds 发明人:YOUNG MICHAEL C; KAPOOR MOHIT 权利人:UNIV TOLEDO 摘要:Methods of synthesizing compounds using CO 2 as a directing group for C—H functionalization, and compounds made thereby, are described.
专利号:US-4041111-A 优先权日:1975-03-04 标题:Phosphonate monoesters and method of preparation 发明人:KELLY SUSAN J; BUTLER LARRY G 权利人:PURDUE RESEARCH FOUNDATION 摘要:Synthesis of phosphonate monoesters, as well as the use of such monoesters as substrates for enzymes which normally hydrolyze phosphodiester linkages, and a method for distinguishing between Type I and Type II phosphodiesterase enzymes using such monoesters as substrates are disclosed herein. Monoesters of phosphonic acids are prepared by the displacement of chloride from an appropriate phosphonic acid dichloride by a phenol or alcohol with pyridine as the solvent, reacting the same and then removing the solvent, after which the remaining ester chloride and dichloride are hydrolyzed by addition of water. The acid and ester are then separated and the acid-free ester is taken up in a polar organic solvent and precipitated as a salt by the addition of aqueous base, with the product then being filtered, washed with fresh acetone, dried and then stored until needed. The thus formed phosphonate monoesters are shown to be effective for use as substrate for phosphodiesterase of the Type I specificity and are shown to be ineffective for use as substrates for phosphodiesterase of the Type II specificity. The type of phosphodiesterase is therefore determined by the amount of activity against phosphonate monoesters.
专利号:WO-2015131100-A1 优先权日:2014-02-28 标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.
专利号:US-2019185392-A1 优先权日:2017-12-20 标 题 :Carbon Dioxide as a Directing Group for C-H Functionalization Reactions Involving Lewis Basic Amines, Alcohols, Thiols, and Phosphines for the Synthesis of Compounds