156453-52-0

Upstream product

• 51699-49-1 3-hydroxy-3-phenylpropyl 4-methylbenzenesulfonate 
• 4850-49-1 1-phenyl-1,3-propanediol 
• 5764-85-2 Ethyl 3-hydroxy-3-phenylpropanoate 
• 96854-34-1 (S)-3-phenyl-1,3-propanediol 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 872850-25-4 (1S)-3-[4-methyl-4-(2-{[4-(methylsulfonyl)phenyl]sulfonyl}ethyl)piperidin-1-yl]-1-phenylpropan-1-ol 
• 718637-43-5 2-{1-[(3R)-3-chloro-3-phenylpropyl] piperidin-4-yl}-N-[4-fluorophenyl]acetamide 
• 1180003-09-1 (S)-6-phenyl-3-m-tolyl-1,3-oxazinan-2-one 
• 1359738-95-6 C₃₁H₄₃F₃N₄O₅S₂ 
• 1359738-94-5 C₃₀H₄₁F₃N₄O₅S₂ 
• 1359738-92-3 C₂₅H₃₃ClN₂O₃S 
• 1180003-27-3 (S)-3-(m-tolylamino)-1-phenyl-propan-1-ol 
• 868669-83-4 (1S)-3-[4-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl]-1-phenylpropan-1-ol 
• 718637-51-5 2-{1-[(3S)-3-hydroxy-3-phenylpropyl]piperidin-4-yl}-N-[4-fluorophenyl]acetamide 
• 718610-69-6 (S)N-(3-hydroxy-3-phenylpropyl)-4-[2-(4-fluorophenylsulphonyl)ethyl]-piperidine 

Relevant academic research and scientific papers

Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase type 1

Structure based design led directly to 1,3-oxazinan-2-one 9a with an IC50 of 42 nM against 11β-HSD1 in vitro. Optimization of 9a for improved in vitro enzymatic and cellular potency afforded 25f with IC 50 values of 0.8 nM for the enzyme and 2.5 nM in adipocytes. In addition, 25f has 94% oral bioavailability in rat and >1000× selectivity over 11β-HSD2. In mice, 25f was distributed to the target tissues, liver, and adipose, and in cynomolgus monkeys a 10 mg/kg oral dose reduced cortisol production by 85% following a cortisone challenge.

INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1

This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-lj1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

The invention provides heteroarylene substituted 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, A, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at th

Pd-catalyzed kinetic resolution of benzylic alcohols: A practical synthesis of (R)-tomoxetine and (S)-fluoxetine hydrochlorides

A convenient synthetic route to (R)-tomoxetine hydrochloride (90% ee) and (S)-fluoxetine hydrochloride (84% ee) is described. (S)-3-Phenyl-3-hydroxypropyl p-toluenesulphonate, the key intermediate, is obtained by the oxidative kinetic resolution of the corresponding racemic 3-phenyl-3-hydroxypropyl p-toluenesulphonate using (-)-sparteine/Pd(II)/O2 (1 atm) catalytic system.