82408-64-8

Upstream product

• 1197-21-3 phentermine hydrochloride 
• 122-09-8 Phentermin 
• 100-52-7 benzaldehyde 
• 34405-42-0 α-(1-amino-1-methylethyl)benzenemethanol 
• 33687-74-0 1-phenyl-2-methyl-2-nitropropanol 
• 26187-18-8 2-chloro-N-(2-methyl-1-phenylpropan-2-yl)acetamide 
• 100-86-7 2-Methyl-1-phenyl-2-propanol 

Downstream Products

• 85135-38-2 15-(2-nitrobenzyl)carazolol 
• 82408-66-0 (+/-)-15-(4-nitrobenzyl)carazolol 
• 454219-23-9 N'-[4-[2-[[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino]-2-methylpropyl]phenyl]-N,N-dimethyl-sulfamide 
• 454219-03-5 4-{2(R)-[2-(tert-butyl-dimethyl-silanyloxy)-2-pyridin-3-yl-ethylamino]-2-methyl-propyl}-phenylamine 
• 454219-32-0 N-[4-[2-[[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino]-2-methylpropyl]phenyl]-N'-(2-methoxyethyl)-sulfamide 
• 454219-22-8 N-[4-[2-[[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino]-2-methylpropyl]phenyl]-N'-phenyl-sulfamide 
• 454219-16-0 N-[4-[2-[[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino]-2-methylpropyl]phenyl]-4-methyl-1-piperidinesulfonamide 
• 454219-15-9 N-[4-[2-[[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino]2-methylpropyl]phenyl]-2,6-dimethyl-,(2R,6S)-4-morpholinesulfonamide 
• 454219-17-1 N-[4-[2-[[(2R)-2-hydroxy-2-(3-pyridinyl)ethyl]amino]2-methylpropyl]phenyl]-3,5-dimethyl-, (3R,5S)-1-piperidinesulfonamide 
• 51131-55-6 4-(β-amino-isobutyl)-aniline 
• 454218-98-5 1(R)-(3-chloro-phenyl)-2-[1,1-dimethyl-2-(4-nitro-phenyl)-ethylamino]-ethanol 
• 180081-15-6 tert-butyl N-[2-methyl-1-(4-nitrophenyl)-2-propyl]carbamate 

Relevant academic research and scientific papers

Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Preparation of Substituted Tetrahydroisoquinolines by Pd(II)-Catalyzed NH2-Directed Insertion of Michael Acceptors into C-H Bonds Followed by NH2-Conjugated Addition

3,3-Disubstituted tetrahydroisoquinolines are prepared in one step from Michael acceptors and 2-phenylethylamines under Pd catalysis and Ag2CO3 as an oxidant. Presumably, activation of an ortho C-H bond of the aromatic ring with Pd(II) is directed by the primary amine to form a palladacycle. Insertion of the olefin, subsequent conjugated addition of the amine, and reductive elimination of Pd(0) affords the expected products. Silver carbonate is not necessary when 2-phenylethylamines are converted previously to N-benzoyloxy-2-phenylethylamines.

A multivalent approach to the discovery of long-acting β2- adrenoceptor agonists for the treatment of asthma and COPD

A multivalent approach was applied to the design of long-acting inhaled β2-adrenoceptor agonists. A series of dimeric arylethanolamines based on the short acting β2-adrenoceptor agonist albuterol were prepared, varying the nature and length of the linker between the basic nitrogens. None of the C2-symmetric dimers demonstrated increased potency, however dimer 5j, derived from 4-phenethylamine, was found to have increased binding potency in vitro relative to the parent monomer. Optimization of this structure led to the identification of 22 (milveterol) which demonstrates high potency in vitro and long duration of action in a guinea pig model of bronchoprotection.

Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design

Previously reported pentapeptidic BACE1 inhibitors, designed using a substrate-based approach, were used as lead compounds for the further design of non-peptidic BACE1 inhibitors. Although these peptidic and non-peptidic inhibitors, with a hydroxymethylcarbonyl isostere as a substrate transition-state mimic, exhibited potent BACE1 inhibitory activities, their molecular-sizes appeared a little too big (molecular weight of >600 daltons) for developing practical anti-Alzheimer's disease drugs. To develop lower weight BACE1 inhibitors, a series of tripeptidic BACE1 inhibitors were devised using a design approach based on the conformation of a virtual inhibitor bound to the BACE1 active site, also called 'in-silico conformational structure-based design'. Although these tripeptidic BACE1 inhibitors contained some natural amino acid residues, they are expected to be useful as lead compounds for developing the next generation BACE1 inhibitors, due to their low molecular size and unique structural features compared with previously reported inhibitors.

Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.

Aryl aniline derivatives as beta2 adrenergic receptor agonists

The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic

Aniline derivatives possessing an inhibitory effect of nitric oxide synthase

Compounds represented by the general formula (1): ? (where R1is SR6or NR7R8, where R6is typically an alkyl group having 1-6 carbon atoms, R7is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2and R3are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3and Y4which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof. The compounds possess a potent nitric oxide synthase inhibiting activity and are useful as therapeutics of cerebrovascular diseases.