57477-80-2

Upstream product

• 98-54-4 para-tert-butylphenol 
• 80783-62-6 N-Trifluoromethyl-N-nitrosobenzenesulfonamide 
• 444-30-4 2-(trifluoromethyl)phenol 
• 75-65-0 tert-butyl alcohol 
• 887144-97-0 Togni's reagent 
• 1961266-44-3 2,8-difluoro-5-(trifluoromethyl)-5H-dibenzo[b,d]thiophen-5-ium trifluoromethanesulfonate 
• 887144-94-7 Togni's reagent II 
• 5787-50-8 sodium 4-tert-butylphenolate 
• 99964-09-7 N-trifluoromethyl-N-nitrosotrifluoromethanesulfon-amide 

Downstream Products

• 57477-83-5 2-hydroxy-3-trifluromethyl-5-(1,1-dimethylethyl)benzaldehyde 
• 61626-87-7 2-aminomethyl-4-(1,1-dimethyl-ethyl)-6-trifluoromethylphenol 
• 57477-82-4 2-aminomethyl-4-tertbutyl-6-trifluoromethylphenol hydrochloride 
• 57477-84-6 3-trifluoromethyl-5-tert-butyl salicylaldehyde oxime 
• 502623-74-7 C₁₃H₁₈F₃O₄P 
• 953091-09-3 (4-tert-butyl-2-trifluoromethyl-phenoxy)-acetic acid ethyl ester 
• 59019-04-4 2-(2-Chloracetamidomethyl)-4-tert.-butyl-6-trifluormethyl-phenol 

Relevant academic research and scientific papers

Simple Photo-Induced Trifluoromethylation of Aromatic Rings

The trifluoromethylation of various aromatic compounds with Umemoto reagent II (2,8-difluoro-5-(trifluoromethyl)-5 H -dibenzo[ b, d ]thiophen-5-ium triflate) proceeded in moderate to good yields under simple photo-irradiation conditions without any cataly

Electrophilic trifluoromethylation of arenes and N-heteroarenes using hypervalent iodine reagents

The reaction of hypervalent iodine trifluoromethylating reagents with a variety of arenes and N-heteroarenes gives access to the corresponding trifluoromethylated compounds. In comparative studies, 1-trifluoromethyl-1,3- dihydro-3,3-dimethyl-1,2-benziodoxole (2) proved to be the superior to 1-trifluoromethyl-1,2-benziodoxol-3-(1H)-one (1) for the direct aromatic trifluoromethylation. Depending on the individual substrates, additives such as zinc bis(trifluoromethylsulfonyl)imide or tris(trimethylsilyl)silyl chloride proved helpful in promoting the reactions. In the case of nitrogen heterocycles a pronounced tendency for the incorporation of the trifluoromethyl group at the position adjacent to nitrogen was observed.

Syntheses and bioactivity of o- or p-trifluoromethylphenyl phosphates

o- and p-Trifluoromethylphenyl phosphates designed as mechanism-based phosphotyrosine phosphatase inactivators have been prepared. Some of them show herbicidal activities.

Reactivity of a 10-I-3 hypervalent iodine trifluoromethylation reagent with phenols

(Chemical Equation Presented) The reaction of the 10-I-3 hypervalent iodine electrophilic trifluoromethylation reagent 1-trifluoromethyl-1,2-benziodoxol-3- (1H)-one (2) with 2,4,6-trimethylphenol, after deprotonation with NaH and in the presence of 18-crown-6 in a polar, nonprotic solvent, affords 1,3,5-trimethyl-2-(trifluoromethoxy)benzene (4) only as a byproduct. Trifluoromethylation occurs preferentially at the ortho- and para-positions of the aromatic core, giving the corresponding trifluoromethylcyclohexadienones 5 and 6. In case the ortho-and/or para-positions are not substituted, the corresponding products of an aromatic, electrophilic substitution are obtained in moderate yield, for example, 2-trifluoromethyl-4-tert-butylphenol (10a) from 4-tert-butylphenol (10).

NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, inflammatory disease of the joints, neuropathies, HIV-related neuropathy, nerve injury, neurodegeneration, stroke, urinary bladder hypersensitivity including urinary incontinence, cystitis, stomach duodenal ulcer, irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD), fecal urgency, gastro-esophageal reflux disease (GERD), Crohn's disease, asthma, chronic obstructive pulmonary disease, cough, neurotic/allergic/inflammatory skin disease, psoriasis, pruritus, prurigo, irritation of skin, eye or mucous membrane, hyperacusis, tinnitus, vestibular hypersensitivity, episodic vertigo, cardiac diseases such as myocardial ischemia, hair growth-related disorders such as effluvium, alopecia, rhinitis, and pancreatitis.

Synthesis and Reactivity of N-Trifluoromethyl-N-nitrosotrifluoromethanesulfonamide as a New Type of Trifluoromethylating Agent

N-Trifluoromethyl-N-nitrosotrifluoromethanesulfonamide (TNS-Tf) was synthesized in a 58 percent yield by the reaction of trifluoronitrosomethane with hydroxylamine followed by the treatment with trifluoromethanesulfonyl fluoride in the presence of a base.TNS-Tf was demonstrated to be an effective trifluoromethylating agent photochemically or thermally for aromatics, thiols, disulfides, and uridine derivatives.The insertion reaction by two trifluoromethyl groups of TNS-Tf to the sulfur-sulfur bonds was observed in the reaction with disulfides having electron-withdrawing groups, giving 2 mols of trifluoromethylthio compounds.Furthermore, TNS-Tf served as a good reagent for mild and convenient in situ generation of trifluoromethylcopper complex which converted iodoaromatics to trifluoromethyl-substituted aromatics in good yields.Similarly, N-trifluoromethyl-N-nitrosononafluoro-1-butanesulfonamide (TNS-Nf) was synthesized in a 36 percent yield.The examination of the reactivity indicated that this type of N-nitroso sulfonamides became to be sources of both perfluoroalkyl radicals contained.

N-TRIFLUOROMETHYL-N-NITROSOBENZENESULFONAMIDE. A NEW TRIFLUOROMETHYLATING AGENT.

N-Trifluoromethyl-N-nitrosobenzenesulfonamide was synthesited.It was demonstrated that it acted as a new trifluoromethylating agent.

2-(Aminomethyl)phenols, a new class of saluretic agents. I. Effect of nuclear substitution

A series of 2-(aminomethyl)phenols was synthesized and tested in rats and dogs for saluretic and diuretic activity. A number of these compounds exhibit a high order of activity on iv or po administration. The most active compounds belong to a subseries of 4-alkyl-6-halo derivatives of which 2,2(aminomethyl)-4-(1,1-dimethylethyl)-6-iodophenyl, is the most active. Compound 2 also possesses significant antihypertensive activity, an adjunctive pharmacological parameter which distinguishes 2 from the other compounds prepared in this series. In addition, 2 displays both topical saluretic and antiinflammatory activities.

3,4-Dihydrospiro-2H-1,3-benzoxazines and their use in treating edema, abnormal electrolyte retention, and inflammation

3,4-Dihydrospiro-2H-1,3-benzoxazines are prepared by condensing aminomethylphenols with cyclic ketones. The products are diuretic and anti-inflammatory agents, and are useful in the treatment of autoimmune diseases, such as multiple sclerosis.

Method of treating autoimmune diseases

3,4-Dihydrospiro-2H-1,3-benzoxazines and pharmaceutical compositions thereof are useful in the treatment of autoimmune diseases.