1349829-79-3

Upstream product

• 1349828-96-1 (2R,5R)-2-methyl-5-phenylmorpholine 
• 127446-34-8 N-(6-chloro-3-formylpyridin-2-yl)-2,2-dimethylpropionamide 
• 1436416-07-7 (2S,5R)-2-chloro-N-(2-hydroxy-1-phenylethyl)propanamide 
• 957121-51-6 (2R,5R)-2-chloro-N-(2-hydroxy-1-phenylethyl)propanamide 
• 86847-84-9 2,2-Dimethyl-N-(6-chloro-2-pyridinyl)propanamide 
• 56613-80-0 D-2-phenylglycinol 
• 957121-52-7 (2R,5R)-2-methyl-5-phenylmorpholin-3-one 
• 1240349-81-8 2-chloro-N-((R)-2-hydroxy-1-phenylethyl)propionamide 

Downstream Products

• 1349829-77-1 6-((2R,5R)-2-methyl-5-phenylmorpholino)-2H-pyrido[3,2-b]-[1,4]oxazin-3(4H)-one 
• 1349829-83-9 ethyl 2-(6-((2R,5R)-2-methyl-5-phenylmorpholino)-2-pivalamidopyridin-3-yloxy)acetate 
• 1349829-96-4 6-[(2R,5R)-2-methyl-5-phenylmorpholin-4-yl]-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine 
• 1349829-81-7 N-(3-hydroxy-6-((2R,5R)-2-methyl-5-phenylmorpholino)pyridin-2-yl)pivalamide 
• 1349830-57-4 7-fluoro-6-((2R,5R)-2-methyl-5-phenylmorpholino)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one 
• 1349831-04-4 6-((2R,5R)-2-methyl-5-phenylmorpholino)-3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine-7-carbonitrile 
• 1349831-06-6 7-bromo-6-((2R,5R)-2-methyl-5-phenylmorpholino)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one 

Relevant academic research and scientific papers

Synthesis of a cis 2,5-disubstituted morpholine by de-epimerization: Application to the multigram scale synthesis of a mineralocorticoid antagonist

A convergent route to multigram quantities of a mineralocorticoid antagonist 3 is described. Starting from (R)-phenylglycinol, the synthesis of cis 2,5-morpholine 2 is accomplished utilizing a de-epimerization to install the second stereogenic center. The multigram synthesis of 3 was completed through a sequence of an SNAr reaction, Dakin oxidation, alkylation, and cyclization to provide a crystalline solid.

MORPHOLINE COMPOUNDS

Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.