181190-33-0

Upstream product

• 383-63-1 ethyl trifluoroacetate, 
• 65854-91-3 N-(4-chlorophenyl)-2,2-dimethylpropionamide 
• 407-25-0 trifluoroacetic anhydride 
• 106-47-8 4-chloro-aniline 
• 1150561-03-7 N-[2-(trifluoroacetyl)phenyl]-2,2-dimethylpropionamide 
• 62662-74-2 N-(2-chlorophenyl)-2,2,2-trimethylacetamide 
• 3282-30-2 pivaloyl chloride 
• 95-51-2 o-chloroaniline 
• 154598-53-5 1-(2-amino-5-chloro-phenyl)-2,2,2-trifluoro-ethanone 
• 18437-66-6 N-(t-butoxycarbonyl)-4-chloroaniline 
• 360-95-2 2,2,2-Trifluoro-1-morpholin-4-yl-ethanone 
• 431-47-0 trifluoroacetic acid-methyl ester 

Downstream Products

• 154598-53-5 1-(2-amino-5-chloro-phenyl)-2,2,2-trifluoro-ethanone 
• 177530-94-8 (S)-N-(4-chloro-2-(4-cyclopropyl-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl)phenyl)pivalamide 
• 177530-95-9 (R)-N-(4-chloro-2-(4-cyclopropyl-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl)phenyl)pivalamide 
• 214353-17-0 4-chloro-2-trifluoroacetylaniline hydrochloride hydrate 
• 177530-96-0 N-[4-chloro-2-(4-cyclopropyl-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl)phenyl]pivalamide 
• 173676-59-0 1-(2-amino-5-chlorophenyl)-2,2,2-trifluoroethanone hydrochloride 
• 177530-93-7 rac-efavirenz 
• 168834-43-3 6-amino-3-chloro-α-cyclopropylethynyl-α-(trifluoromethyl)benzyl alcohol 
• 154598-52-4 efavirenz 

Relevant academic research and scientific papers

Benzylidene succinimides as 3C synthons for the asymmetric tandem Mannich reaction/transamidation of cyclic trifluoromethyl ketimines to obtain F3C-containing polycyclic dihydroquinazolinones

By taking advantage of benzylidene succinimides as a new class of 3C synthons, a highly diastereo- and enantioselective tandem Mannich reaction/transamidation has been established by reacting them with cyclic trifluoromethylN-acyl ketimines. Using aCinchonaalkaloid-derived squaramide as the catalyst, the tandem reaction proceeded smoothly under mild conditions and afforded a range of F3C-containing chiral polycyclic dihydroquinazolinones with excellent results (up to 99% yield, all cases >20?:?1 dr, up to 99% ee).

Construction of CF3-containing tetrahydropyrano[3,2- b]indoles through DMAP-catalyzed [4+1]/[3+3] domino sequential annulation

A [4+1]/[3+3] domino sequential annulation reaction of o-aminotrifluoroacetophenone derivatives and β′-acetoxy allenoates enabled by DMAP has been reported. A variety of CF3-containing tetrahydropyrano[3,2-b]indoles were obtained as a single diastereomer in high yields (≤98%) under mild conditions. The reaction can build one C-N bond, one C-C bond, and one C-O bond sequentially in a single step. The synthetic utility was demonstrated with gram-scale reactions and various transformations of the products.

A preparing method of an efavirenz intermediate

The invention provides a preparing method of an efavirenz intermediate, and relates to the technical field of compound preparation methods. The method includes performing amino protection on 2-halogenaniline (II), as a raw material, with acyl chloride; reacting the generated N-acyl-2-halogen-aniline (III) with metal magnesium to generate a Grignard reagent; then reacting the Grignard reagent witha trifluoroacetyl amine compound (IV) to obtain N-acyl-2-(trifluoroacetyl)aniline (V); then reacting the N-acyl-2-(trifluoroacetyl)aniline (V) with chlorine under the function of a catalyst to obtainN-acyl-4-chloro-2-(trifluoroacetyl)aniline (VI); and performing hydrolysis and salting to obtain 4-chloro-2-(trifluoroacetyl)aniline hydrochloride hydrate (I). The method has characteristics of shortsynthetic steps, simple operation, high safety, a large raw material choosing range, and a high yield of the target product, and is suitable for large-scale industrial production.

Preparation method of 4-chloro-2-(trifluoroacetyl) aniline hydrochloride hydrate

The invention discloses a preparation method of a 4-chloro-2-(trifluoroacetyl) aniline hydrochloride hydrate and belongs to the field of compound synthesis. The method adopts parachloroaniline as a raw material and comprises steps as follows: 1, parachlor

Asymmetric autocatalysis enables an improved synthesis of efavirenz

(Chemical Equation Presented) Priming the pump: An asymmetric autocatalytic zinc acetylide addition employs catalytic amounts of the enantiomerically pure product as part of a chiral cocktail. This new strategy enables an improved synthesis of a key precursor to efavirenz (see scheme).

Trifluoromethyl-promoted homocamptothecins: Synthesis and biological activity

The homocamptothecin (hCPT) represents a new class of topoisomerase inhibitor which combines enhanced plasma stability and strong antitumor activity. Fluorine imparts desirable characteristics to drugs by modulating both the pharmacokinetics and pharmacodynamic properties of a drug. Therefore, in an attempt to improve the antitumor activity of homocamptothecins, seven new 7-trifluoromethylated homocamptothecin derivatives were prepared by proline-catalyzed Friedlander annulation. The antitumor activity in vitro and in vivo on cancer cell lines, and inhibitory properties of topoisomerase I-mediated DNA cleavage of compounds 6c and 8b were evaluated. Several of these trifluoromethylated hCPT derivatives (such as 6a, 6b and 6c) possessed higher in vitro antitumor activity than topotecan (TPT). Especially, the compound 6c showed effective in vivo antitumor activity comparable to that of TPT.

An alternative route for synthesis of o-trifluoroacetylanilines as useful fluorine-containing intermediates

A series of o-trifluoroacetyl aniline derivatives were synthesized in three steps. In this method, we first utilized trifluoroacetic anhydride to introduce trifluoroacetyl group to the ortho position of aniline with higher yield than that of some previously reported methods. In addition, the procedure is shown to be highly regiospecific. This type of compounds can be used as the key intermediates in the preparation of a variety of inhibitors of HIV reverse transcriptase which is an important pharmacological target of many anti-AIDS agents.

Substituted Nitrogen Heterocycles and Synthesis and Uses Thereof

The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.

QUINAZOLINONE T-TYPE CALCIUM CHANNEL ANTAGONISTS

The present invention is directed to quinazolinone compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

INDOLES USEFUL IN THE TREATMENT OF INFLAMATION

There is provided compounds of formula (I), Wherein T, Y, X1 , R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.