130972-89-3

Usage

Uses

Used in Pharmaceutical Industry:
Tert-butyl 4-hydroxy-3-methoxybenzylcarbamate is used as a pharmaceutical intermediate for the synthesis of various pharmaceutical substances, contributing to the development of drugs for different therapeutic applications.
Used as an Antioxidant or Stabilizer:
Due to its hydroxy and methoxy groups, tert-butyl 4-hydroxy-3-methoxybenzylcarbamate is used as an antioxidant or stabilizer in certain products, enhancing their shelf life and performance.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 7149-10-2 vanillylamine hydrochloride 
• 81259-54-3 4-benzyloxy-3-methoxybenzaldehyde oxime 
• 1196-92-5 Vanillylamin 

Downstream Products

• 130972-90-6 tert-butyl N-[4-(2-bromoethoxy)-3-methoxybenzyl]carbamate 
• 944256-01-3 C₁₅H₂₃NO₄ 
• 1220703-52-5 (1R,2S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-((tert-butoxycarbonyl){[4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)biphenyl-2-yl]methyl}amino)propyl-4-{[(tert-butoxycarbonyl)amino]methyl}-2-methoxyphenylcarbonate 
• 130972-80-4 N-[4-(2-aminoethoxy)-3-methoxybenzyl]-N'-[2-(4-chlorophenyl)ethyl]thiourea 
• 1026883-06-6 [2-(4-{3-[2-(4-Chloro-phenyl)-ethyl]-thioureidomethyl}-2-methoxy-phenoxy)-ethyl]-methyl-carbamic acid 9H-fluoren-9-ylmethyl ester 
• 139693-28-0 1-(3,5-Di-tert-butyl-benzyl)-3-{4-[2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-ethoxy]-3-methoxy-benzyl}-thiourea 
• 1026821-70-4 {2-[4-(tert-Butoxycarbonylamino-methyl)-2-methoxy-phenoxy]-ethyl}-methyl-carbamic acid 9H-fluoren-9-ylmethyl ester 
• 184003-42-7 1-[2-(2,4-Dichloro-phenyl)-ethyl]-3-{4-[2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-ethoxy]-3-methoxy-benzyl}-thiourea 
• 184003-56-3 1-[2-(4-tert-Butyl-phenyl)-ethyl]-3-{4-[2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-ethoxy]-3-methoxy-benzyl}-thiourea 
• 184003-52-9 1-{4-[2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-ethoxy]-3-methoxy-benzyl}-3-(4-trimethylsilanyl-benzyl)-thiourea 
• 184003-61-0 1-[2-(4-Chloro-phenyl)-ethyl]-3-{4-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propoxy]-3-methoxy-benzyl}-thiourea 
• 139693-29-1 1-(4-tert-Butyl-benzyl)-3-{4-[2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-ethoxy]-3-methoxy-benzyl}-thiourea 
• 130972-94-0 N-[4-(2-Phthalimidoethoxy)-3-methoxybenzyl]-N'-[2-(4-chlorophenyl)ethyl]thiourea 
• 184003-39-2 1-{4-[2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-ethoxy]-3-methoxy-benzyl}-3-[2-(4-fluoro-phenyl)-ethyl]-thiourea 

Relevant academic research and scientific papers

Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus

To address the emergency caused by multi-drug resistant Staphylococcus aureus, a series of novel capsaicin derivatives with nitrothiophene substituents have been designed and evaluated for the antibacterial activities against S. aureus Newman and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). The structure-activity relationship was further revealed. Compound 13c, 13f, and 13g were highly active against staphylococcal growth, with minimal inhibition concentration (MIC) values of 0.39–1.56 μg/mL. The oxadiazole-derived compound 21, a bioisostere of ester 13f, is the most potent candidate for anti-growth of five multidrug-resistant S. aureus strains with MICs of 0.20–0.78 μg/mL, which is more active compared with vancomycin in vitro. Notably, these anti-staphylococcal compounds are much less cytotoxic to the normal kidney epithelial cell line (HK293T).

I. Discovery of a novel series of CXCR3 antagonists. Multiparametric optimization of N,N-disubstituted benzylamines

N,N-Disubstituted benzylamine derivatives have been identified as CXCR3 antagonists. Compounds were optimized to improve affinity and selectivity, to increase metabolic stability in human and mouse liver microsomes, to increase Caco-2 permeability. Optimization was supported by monitoring physico-chemical properties using both experimental and computational means. Several compounds with double-digit nanomolar CXCR3 affinity, favorable selectivity, microsomal stability, Caco-2 permeability and human hepatocyte clearance have been identified.

The SAR analysis of TRPV1 agonists with the α-methylated B-region

A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogues were investigated. Whereas the α-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The analysis indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.

PRODRUGS OF OXAZOLIDINONE CETP INHIBITORS

The compounds of Formula I are prodrugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.

UROTENSIN II RECEPTOR ANTAGONISTS

The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.

Vanilloid analogues containing resinferatoxin pharmacophores as potent vanilloid receptor agonists and analgesics, compositions and uses thereof

The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.

Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics

In order to improve the analgesic activity and pharmacokinetics of thioureas 2 and 3, which we previously developed as potent vanilloid receptor (VR) agonists, we prepared and characterized phenolic modifications of them and of their amide surro-gates (7, 8). The aminoethyl analogue of the amide template 13 was a potent analgesic with an EC50 =0.96 μg/kg in the AA-induced writhing test and with better in vivo stability than the parent phenol. Copyright

One-pot conversion of oximes to N-(tert-butoxycarbonyl) amines with polymethylhydrosiloxane, Pd-C and di-tert-butyl dicarbonate

N-(tert-butoxycarbonyl) amines are directly obtained from oximes of aldehydes and ketones in one-pot when treated with polymethylhydrosiloxane (PMHS) and di-tert-butyl dicarbonate in the presence of catalytic amount of 10% Pd-C for the first time.

Analogues of capsaicin with agonist activity as novel analgesic agents: Structure-activity studies. 4. Potent, orally active analgesics

Structural features of three regions of the capsaicin molecule necessary for agonist properties were delineated by a previously reported modular approach. These in vitro agonist effects were shown to correlate with analgesic potency in rodent models. Comb

Capsaicin derivatives

Novel capsaicin derivatives of general formula I STR1 wherein R, R1 to R7 and X may be a variety of substituents, processes for the production thereof, pharmaceutical compositions containing them and use thereof as pharmaceuticals.