379222-83-0

Upstream product

• 231623-74-8 N-(7-methoxy-3,4-dihydro-naphthalen-2-yl)-benzamide 
• 231623-76-0 N-[(2S)-7-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl]benzamide 
• 85951-60-6 (-)-7-OH-AT 
• 4133-34-0 7-methoxyl-2-tetralone 
• 603122-70-9 (7S)-7-(benzylamino)-5,6,7,8-tetrahydronaphthalen-2-ol 
• 132990-84-2 (2S)-N-benzyl-7-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine 
• 194785-39-2 benzyl [(2S)-7-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate 
• 358-23-6 trifluoromethylsulfonic anhydride 

Downstream Products

• 379222-84-1 (2S)-2-benzyloxycarbonylamino-7-(3-ethoxy-3-oxo-1-propenyl)-tetralin 
• 603122-34-5 methyl 4-((7S)-7-{[(benzyloxy)carbonyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603122-35-6 methyl 4-((7S)-7-{[(benzyloxy)carbonyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603122-42-5 methyl 4-((7S)-7-{[(2R)-2-(4-chlorophenyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603122-44-7 sodium 4-((7S)-7-{[(2R)-2-(4-chlorophenyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603125-42-4 sodium 4-((7S)-7-{[(2R)-2-(2-chlorophenyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603125-44-6 sodium 4-((7S)-7-{[(2R)-2-(4-cyanophenyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603125-43-5 sodium 4-((7S)-7-{[(2R)-2-(4-trifluoromethylphenyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603125-45-7 sodium 4-((7S)-7-{[(2R)-2-(3,4-dichlorophenyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603124-73-8 sodium 4-((7S)-7-{[(2R)-2-(6-chloro-3-pyridinyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoate 
• 603123-08-6 methyl 4-[(7S)-7-{(tert-butoxycarbonyl)[(2R)-2-hydroxy-2-(4-methylphenyl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-2-yl]benzoate 
• 603122-47-0 methyl 4-((7S)-7-{(tert-butoxycarbonyl)[(2R)-2-(6-chloro-3-pyridinyl)-2-hydroxyethyl]amino}-5,6,7,8-tetrahydro-2-naphtahlenyl)benzoate 
• 603122-48-1 C₂₉H₃₁ClN₂O₅ 
• 603122-50-5 4-((7S)-7-{(tert-butoxycarbonyl)[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino}-5,6,7,8-tetrahydro-2-naphthalenyl)benzoic acid 

Relevant academic research and scientific papers

Discovery of a novel series of benzoic acid derivatives as potent and selective human β3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety

We designed a series of benzoic acid derivatives containing the biphenyl ether or biphenyl template on the RHS and a phenylethanolaminotetraline (PEAT) skeleton, which was prepared by highly stereoselective synthesis, to generate two structurally different lead compounds (10c, 10m) with a good balance of potency, selectivity, and pharmacokinetic profile. Further optimization of the two lead compounds to improve potency led to several potential candidates (i.e., 11f, 11l, 11o, 12b). In particular, biphenyl analogue 12b exhibited an excellent balance of high potency (EC50 = 0.38 nM) for β3, high selectivity over β1 and β2, and good pharmacokinetic properties in rats, dogs, and monkeys.

Propanolaminotetralines, preparation thereof and compositions containing same

The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.