33577-83-2

Upstream product

• 27914-73-4 4-acetoxybenzoyl chloride 
• 62-53-3 aniline 

Downstream Products

• 102827-03-2 (4-(dimethylamino)phenyl)(4-hydroxyphenyl)methanone 
• 14121-97-2 4-hydroxybenzanilide 

Relevant academic research and scientific papers

Aryl alkyl ether compound as well as derivative, preparation method, pharmaceutical composition and application thereof

The invention discloses an aryl alkyl ether compound as well as a derivative, a preparation method, a pharmaceutical composition and application thereof. The structure of the aryl alkyl ether compound is shown as a formula (I). The aryl alkyl ether compound derivative relates to a stereoisomer, a tautomer, a metabolite, a metabolic precursor, a prodrug, a solvate, a salt of the solvate, a crystal, a pharmaceutically acceptable salt or a mixture of the stereoisomer, the tautomer, the metabolite, the metabolic precursor, the prodrug and the solvate of the aryl alkyl ether compound. The aryl alkyl ether compound and the derivative thereof have a remarkable inhibition effect on indoleamine 2, 3-dioxygenase 1, and can be used for preparing a medicine for treating indoleamine 2, 3-dioxygenase 1 mediated immunosuppression related diseases, and the prepared medicine can exert the medicine effect at the molecular level and is wide in application.

Stannous chloride dihydrate-mediated efficient access to secondary and primary amides from oximes

Highly selective, efficient and expeditious Beckmann rearrangement of a wide range of ketoximes to secondary amides (20 examples) has been accomplished using stoichiometric amount of stannous chloride dihydrate in the presence of nucleophilic additive, tetra-n-butylammonium iodide (TBAI) (10 moI%) and 4 ? MS in dry acetonitrile at reflux temperature. Aldoximes delivered primary amides through intermediacy of nitriles upon heating with an equimolar amount of SnCl2·2H2O and DBU in dry toluene at reflux in good to acceptable yields (12 examples). Utilization of mild Lewis acid, inexpensive rack reagents and procedural simplicity including easy isolation of products are key advantageous features of the protocol.

QUINOLINE AND QUINOXALINE DERIVATIVES AS INHIBITORS OF KINASE ENZYMATIC ACTIVITY

Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, -CH2-, -O-, -S-, -S(=O)2-, or -NR5- where R5 is hydrogen or C1-C4 alkyl; Q is =N-, =CH- or =C(X1)- wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, -(C=O)R3, -(C=O)OR3, or -(C=O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and D is a monocyclic heterocyclic ring of 5 or 6 ring atoms.