53120-53-9

Upstream product

• 700-57-2 1-adamantanol 
• 75-44-5 phosgene 
• 32315-10-9 bis(trichloromethyl) carbonate 

Downstream Products

• 150871-35-5 N-<(2-adamantyloxy)carbonyl>-DL-α-methyl-3-phenylalanine 
• 160516-87-0 Z-His(2-Adoc)-OH 
• 1025903-95-0 {[2-(Adamantan-2-yloxycarbonylamino)-2-methyl-3-naphthalen-2-yl-propionyl]-phenethyl-amino}-acetic acid ethyl ester 
• 176222-67-6 2-(Adamantan-2-yloxycarbonylamino)-3-biphenyl-4-yl-2-methyl-propionic acid methyl ester 
• 130406-44-9 tricyclo<3.3.1.1^3,7>dec-2-yl (S)-<1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-1-<(1-phenylethyl)amino>ethyl>carbamate 
• 130406-43-8 tricyclo[3.3.1.1^3,7]dec-2-yl (R)-{1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2-[(2-phenylethyl)amino]ethyl}carbamate 
• 130406-47-2 PD 132458 
• 135998-75-3 benzyl-(+/-)-β-<<2-(trimethylsilyl)ethoxy>carbonyl>-β-<<(tricyclo<3.3.1.1>dec-2-yloxy)carbonyl>amino>-1H-3-butanoate 
• 134558-12-6 methyl-(+/-)-β-<(phenylmethoxy)carbonyl>-β-<<(tricycl<3.3.1.1>dec-2-yloxy)carbonyl>amino>-1H-indole-3-butanoate 
• 130466-73-8 tricyclo[3.3.1.13,7 ]dec-2-yl [1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2-[(2-phenylethyl)amino]-ethyl]carbamate 
• 1257520-42-5 2-adamantyl 2-phenylpyrrolidine-1-carboxylate 
• 1257520-47-0 2-(1-(2-adamantyloxycarbonyl)-4-O-tolylpiperidin-4-yl)acetic acid 
• 1257520-46-9 1-(2-adamantyl) 4-methyl 4-phenylpiperidine-1,4-dicarboxylate 
• 53120-54-0 Adamantan-2-yl-N-cyclohexylcarbamat 

Relevant academic research and scientific papers

Versatile Cp*Co(III)(LX) Catalyst System for Selective Intramolecular C-H Amidation Reactions

Herein, we report the development of a tailored cobalt catalyst system of Cp*Co(III)(LX) toward intramolecular C-H nitrene insertion of azidoformates to afford cyclic carbamates. The cobalt complexes were easy to prepare and bench-stable, thus offering a convenient reaction protocol. The catalytic reactivity was significantly improved by the electronic tuning of the bidentate LX ligands, and the observed regioselectivity was rationalized by the conformational analysis and DFT calculations of the transition states. The superior performance of the newly developed cobalt catalyst system could be broadly applied to both C(sp2)-H and C(sp3)-H carbamation reactions under mild conditions.

Preparation method of alicyclic and aromatic-aliphatic chloroformate

The invention belongs to the technical field of fine chemistry, and in particular relates to a preparation method of alicyclic and aromatic-aliphatic chloroformate. The preparation method is characterized in that alicyclic alcohol chloroformate or aromatic-aliphatic alcohol chloroformate is obtained by taking alicyclic alcohol or aromatic-aliphatic alcohol and bis(trichlormethyl)carbonate as raw materials, taking organic base as a catalyst and reacting in an organic solvent under certain reaction temperature and certain reaction time, wherein molar ratio among the alicyclic alcohol or the aromatic-aliphatic alcohol, the bis(trichlormethyl)carbonate and the organic base is 1 to (0.4 to 1) to (1.2 to 3); experiment time and experiment temperature are different in two stages, in the first stage, the reaction temperature is -10 to 0 DEG C, and the reaction time is 2 to 5 hours; in the second stage, the reaction temperature is 0 to 25 DEG C, and the reaction time is 7 to 13 hours; a mass ratio between the organic solvent and the alicyclic alcohol or the aromatic-aliphatic alcohol is (10 to 25) to 1; residue in a reaction system is effectively treated, and reaction waste is also recycled and utilized. The preparation method disclosed by the invention has the characteristics of stable reaction, high reaction yield and product purity, environment protection of a reaction process, low production cost, less emission of three wastes, simpleness in preparation technology and easiness in industrialization.

INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1

This invention relates to novel compounds of the Formula (I*), 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

CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1

This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-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.

Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1

Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 9a with an IC50 of 15.2 nM against human 11β-HSD1 in adipocytes. Optimization for increased adipocyte potency, metabolic stability and select

A structural screening approach to ketoamide-based inhibitors of cathepsin K

Several novel ketoamide-based inhibitors of cathepsin K have been identified. Starting from a modestly potent inhibitor, structural screening of P2 elements led to 100-fold enhancements in inhibitory activity. Modifications to one of these leads resulted in an orally bioavailable cathepsin K inhibitor.

N-substituted cycloalkyl and polycycloalkyl α-substituted Trp-Phe- and phenethylamine derivatives

Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.

N-SUBSTITUTED CYCLOALKYL AND POLYCYCLOALKYL ALPHA-SUBSTITUTED TRP-PHE- AND PHENETHYLAMINE DERIVATIVES

Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.

Process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines and derivatives thereof

A process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines is described where N-protected DL-3,3-diphenylalanine or N-protected-DL-substituted 3,3-diphenylalanine are treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.