192815-71-7

Upstream product

• 56613-80-0 D-2-phenylglycinol 
• 105-39-5 chloroacetic acid ethyl ester 
• 94193-77-8 (R)-N-(2-hydroxy-1-phenylethyl)-2-chloroacetamide 
• 79-04-9 chloroacetyl chloride 

Downstream Products

• 192815-73-9 2-Diazo-3-oxo-3-((R)-3-oxo-5-phenyl-morpholin-4-yl)-propionic acid ethyl ester 
• 192815-78-4 (R)-4-(2-Diazo-acetyl)-5-phenyl-morpholin-3-one 
• 957121-46-9 tert-butyl (5R)-3-oxo-5-phenylmorpholine-4-carboxylate 
• 1429228-65-8 (R)-tert-butyl 3-(4-iodophenyl)morpholine-4-carboxylate 
• 138713-44-7 3-(-)-Phenyl morpholine 
• 107-92-6 butyric acid 

Relevant academic research and scientific papers

SUBSTITUTED MORPHOLINE DERIVATIVES AS ROR GAMMA MODULATORS

The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, X1, X2, m and n are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORyt). These compounds prevent, inhibit, or suppress the action of RORyt and are therefore useful in the treatment of RORyt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer. (I)

Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments

Efficient syntheses of chiral fragments derived from chiral amino alcohols are described. Several unique scaffolds were readily accessed in 1-5 synthetic steps leading to 45 chiral fragments, including oxazolidinones, morpholinones, lactams, and sultams. These fragments have molecular weights ranging from 100 to 255 Da and are soluble in water (0.085 to >15 mM).

COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE

The invention relates to the compound 5-(4-isopropylsulfonylphenyl) -3-[3-[4-[(3R)-morpholin-3-yl]phenyl]isoxazol-5-yl]pyrazine-2-amine and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of ATR kinase.

The first enantiomerically pure thiadiazol-3-one 1-oxide and thiatriaza-indene 3-oxide systems chiral at the sulfur atom

The first synthesis of an enantiomerically pure C2 symmetric benzothiadiazole 2-oxide is described along with the first synthesis of an enantiomerically thiadiazol-3-one 1-oxide and a thiatriaza-indene 3-oxide system both chiral at the sulfur a

Cycloadditions of chiral carbonyl ylides with imine dipolarophiles as a route to enantiomerically pure α-amino-β-hydroxy acids

The preparation of enantiomerically pure threo-β-amino-α-hydroxy acids via 1,3-dipolar cycloadditions of imine dipolarophiles with the chiral isomuenchnone derived from (5R)-5-phenylmorpholin-3-one 1 is described. The cycloadducts were obtained with excellent diastereofacial- and exo-selectivity. Subsequent hydrolysis and chemoselective exocyclic amide cleavage afforded the threo-β-amino-α-hydroxy acids with recovery of the initial chiral auxiliary.

4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase

4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.

Substituted monocyclic CGRP receptor antagonists

Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Cycloadditions of 1,3-oxazolium-4-olates (Isomunchnones) by Rhodium(II)-Induced decomposition of α-Diazocarbonyl derivatives of (5R)- and (5S)-phenyloxazin-3-one as a chiral template

Cycloadducts (6-9) were synthesised from isomunchnone derivatives of (5R)- and (5S)-phenyloxazin-3-one by rhodium(II)-catalysed decomposition of α-diazocompounds (3a-c). Additions to various carbon-carbon dipolarophiles proceeded with high endo/exo-selectivities and moderate diastereofacial selectivities.