181640-70-0

Upstream product

• 265998-03-6 {2-[1-(3,4-dichloro-phenyl)-1-iodomethyl-3-trityloxy-propoxy]-ethyl}-carbamic acid tert-butyl ester 
• 265998-02-5 2-(3,4-dichloro-phenyl)-2-(2-trityloxy-ethyl)-morpholine-4-carboxylic acid tert-butyl ester 

Downstream Products

• 299428-12-9 (2R)-2-[4-{[3,5-bis(trifluoromethyl)phenyl]acetyl}-2-(3,4-dichlorophenyl)morpholin-2-yl]ethanol 
• 191673-56-0 (R)-2-(2-(3,4-dichlorophenyl)morpholin-2-yl)ethanol 

Relevant academic research and scientific papers

Heterocyclic compounds having tachykinin receptor antagonist activity their preparation and their use

Compounds of the formula and quaternary ammonium ions thereof, wherein R1 and R2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C1-C4 alkylene or C2-C4, alkenylene; D is oxygen; E is C2 alkylene; G is C1-C4 alkylene or C2-C4 alkenylene; and L is -C(R4)(R5), wherein R4 and R5 together with the carbon atom to which they are attached represent a C5-C10 cycloalkyl or a C5-C10 heterocyclic. Especially preferred are compounds wherein L represents wherein J is a C1-C6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*->O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK1 and NK2 receptors.

Combined tachykinin receptor antagonist: Synthesis and stereochemical structure-activity relationships of novel morpholine analogues

We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 exhibited high binding affinities for NK1, NK2 and NK3 receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

A versatile method for the preparation of 2,2-disubstituted morpholine analogues

We describe a versatile synthetic method for the preparation of 2,2- disubstituted morpholine analogues. Iodo-etherification of 1,1-disubstituted olefin with N-Boc-aminoethanol using NIS proceeded smoothly in a regioselective manner and the following cyclization was accomplished in good yield. We successfully applied this method for the preparation of the key intermediate 2 of tachykinin receptor antagonist. (C) 2000 Elsevier Science Ltd.