- ACETAMIDO DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS
-
Disclosed herein are certain acetamido derivatives that are DNA Polymerase Theta (Polθ) inhibitors of Formula (I). Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
- -
-
Paragraph 0162-0163
(2020/08/22)
-
- Formation of N-heterocycles by the reaction of thiols with glyoxamides: Exploring a connective Pummerer-type cyclisation
-
The reaction of thiols with glyoxamides provides a convenient method for the generation of thionium ions and the initiation of Pummerer-type reactions. When the glyoxamides contain tethered aromatic nucleophiles, N-heterocycles are formed by a thionium ion cyclisation. The scope and mechanism of the connective Pummerer-type process has been investigated using a range of thiols, Lewis acids and both mono- and bis-glyoxamides. The utility of the process has been illustrated in a synthesis of the indoloquinoline natural product, neocryptolepine. The Royal Society of Chemistry 2009.
- Miller, Marc,Vogel, Johannes C.,Tsang, William,Merrit, Andrew,Procter, David J.
-
scheme or table
p. 589 - 597
(2009/07/18)
-
- Benzothiazole substituted carboxylic acid amide compounds and herbicidal methods compositions thereof
-
Novel substituted carboxylic acid amide compound of the formula STR1 wherein n is an integer from 1 to 4 each R is independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, nitro, cyano and alkoxycarbonyl; and two R radicals taken together can represent methylenedioxy, dichloromethylenedioxy or difluoromethylenedioxy, R1 is hydrogen or alkyl, R2 and R3 are individually selected from hydrogen or a radical selected from alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl and nitrogen-containing heterocycles, each of which radicals may be substituted and each of which radicals may, together with the nitrogen atom to which they are attached, form an optionally substituted, optionally partially unsaturated and optionally benzofused monocyclic or bicyclic radical, which may contain one or more further hetero-atoms, and X is oxygen or sulfur.
- -
-
-
- Process for the preparation of alpha-hydroxycarboxylic acid amide compounds
-
Process for the preparation of an alpha-hydroxycarboxylic acid amide compound of the formula STR1 wherein R1 is hydrogen or alkyl; and R2 and R3 are individually selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl or aryl, each of which may be optionally substituted, or a nitrogen-containing heterocyclic radical; or R2 and R3, together with the nitrogen atom to which they are bonded, represent an optionally benzo-fused monocyclic or bicyclic ring, which ring may be substituted and may be partially unsaturated, which process comprises reacting in a first stage an alpha-halocarboxylic acid amide of the formula STR2 wherein R1, R2 and R3 are identified as above; and Hal is chlorine or bromine, with an alkali metal acetate or alkaline earth metal acetate in the presence of a quaternary ammonium salt at a temperature between 20° and 200° C., and, in a second stage, deacylating the alpha-acetoxycarboxylic acid amide produced, having the general formula STR3 in which R1, R2 and R3, are identified as above by reacting said amide III with an alcohol of the general formula in which R4 is alkyl in the presence of a catalytic amount of a catalyst selected from alkali metal hydroxides, alkaline earth metal hydroxides, alkali metal carbonates, and alkaline earth metal carbonates, at a temperature between 20° and 150° C., these compounds are useful as intermediates in the preparation of herbicides, e.g., substituted sulfonyl glycol amides and anilides.
- -
-
-
- Substituted o-[aminosulfonyl]-glycolic anilides
-
New and valuable substituted O-[aminosulfonyl]-glycolic anilides and a process for controlling the growth of unwanted plants with these compounds.
- -
-
-
