2727-71-1

Upstream product

• 615-36-1 2-bromoaniline 
• 407-25-0 trifluoroacetic anhydride 
• 2923-18-4 sodium 2,2,2-trifluoroacetate 
• 404-24-0 2,2,2-trifluoro-N-phenylacetamide 
• 354-32-5 trifluoracetyl chloride 
• 76-05-1 trifluoroacetic acid 

Downstream Products

• 120-72-9 indole 
• 404-24-0 2,2,2-trifluoro-N-phenylacetamide 
• 78839-81-3 (3aS,8bR)-2,3,3a,4-Tetrahydro-1H-cyclopenta[b]indol-8b-ol 
• 130074-91-8 2,2,2-trifluoro-N-<2-(3-methylbut-2-enyl)phenyl>acetamide 
• 78839-85-7 (E)-4-Hydroxy-4-[2-(2,2,2-trifluoro-acetylamino)-phenyl]-but-2-enoic acid methyl ester 
• 139517-16-1 10b-hydroxy-5,5a,6,9-tetrahydroindeno<2,1-b>indole 
• 79892-22-1 cis-dibenzo-1-chloro-8-oxaspiro<7,9>undecan-10-one 
• 134379-28-5 N-[2-(2-Chloro-1-hydroxy-5-methoxy-4,6-dimethyl-indan-1-yl)-phenyl]-2,2,2-trifluoro-acetamide 
• 133571-29-6 5,10-Dihydro-2-methoxy-1,3-dimethylindeno[1,2-b]indole 
• 136282-14-9 5-methoxy-4,6-dimethyl-2-(2'-trifluoroacetamidophenyl)indan-1-one 
• 89424-05-5 3-Chloro-4-hydroxy-4-[2-(2,2,2-trifluoro-acetylamino)-phenyl]-piperidine-1-carboxylic acid ethyl ester 
• 83-34-1 3-Methylindole 
• 942-01-8 1,2,3,4-tetrahydrocarbazole 
• 78839-80-2 2,2,2-Trifluoro-1-((4aS,9aR)-4a-hydroxy-1,2,3,4,4a,9a-hexahydro-carbazol-9-yl)-ethanone 

Relevant academic research and scientific papers

Overcoming inaccessibility of fluorinated imines-synthesis of functionalized amines from readily available fluoroacetamides

Although imines are convenient substrates for the synthesis of functionalized amines, they may be hard to obtain, as in the case of fluorinated imines. To aid in overcoming this issue, we propose a protocol of corresponding amine synthesis from simple fluoroacetic acid-derived amides using Schwartz's reagent.

Ruthenium Amide Complexes – Synthesis and Catalytic Activity in Olefin Metathesis and in Ring-Opening Polymerisation

A set of olefin metathesis catalysts bearing a ruthenium amide moiety was synthesised. In the ruthenium amide form these complexes exhibit very low activity in standard metathesis reactions. However, a dramatic increase of activity was observed upon in si

Palladium-catalyzed carbonylative synthesis of benzoxazinones from N -(o -bromoaryl)amides using paraformaldehyde as the carbonyl source

Carbonylation reactions have been widely used in organic synthesis. However, the manipulation of toxic and pressurized carbon monoxide limited their applications in organic laboratories. The search for alternative carbonyl sources as an important method for carbonylative organic synthesis is spreading. Herein, a series of substituted benzoxazinones were synthesized from N-(o-bromoaryl)amides by palladium-catalyzed carbonylation with paraformaldehyde as the carbonyl source, which is inexpensive, stable, and easy to use. Notably, this is the first example of using paraformaldehyde as the CO source in palladium-catalyzed carbonylative synthesis of heterocycles.

Ruthenium-amido complexes: Synthesis, structure, and catalytic activity in olefin metathesis

Unprecedented amido derivatives of the first-, second-, and third-generation Grubbs ruthenium catalysts were prepared, characterized, and tested in ring-closing metathesis (RCM) of model dienes. In the ruthenium-amide (formally: 2-ruthenaindole) form, the

SYNTHESIS OF SUBSTITUTED PYRAZOLINE CARBOXAMIDINE DERIVATIVES

This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wh

ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.

Synthesis of medium ring heterocycles using an intramolecular Heck reaction

(Equation Presented) Historically, general convergent syntheses of medium ring heterocycles have been difficult to develop. Herein, we describe the synthesis of five classes of heterocycles: dihydrodibenzo[b,f]azepine, -oxocine, and -thiocine and dibenzo[b,f]azepine and -oxepine using a strategy of alkylation followed by highly selective intramolecular Heck arylation reaction. The hetero-tricyclic compounds were available in only two steps starting from commercially available starting materials.

A convenient synthesis of Trifluoroacetamides from sodium trifluoroacetate and amines

Trifluoroacetamides were prepared readily by reaction of sodium trifluoroacetate with triphenylphosphine di-iodide and amines consecutively under mild conditions with good yields.

INDOLE DERIVATIVES

Compounds of the formula STR1 where W is STR2 n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is--O--,--S--,--NH, or--CH 2 ; R 1 is hydrogen, C. sub.1 to C. sub.8 alkyl, substituted C 1 to C 8 alkyl substituted with one hydroxy, C 3 to C 8 alkenyl, C 3 to C 8 alkynyl, aryl, C. sub.1 to C 3 alkylaryl, C 1 to C 3 alkylheteroaryl, or--Q--R. sub.4 ; R 2 and R 3 are each independently hydrogen, C. sub.1 to C. sub.6 alkyl, aryl, C 1 to C 3 alkylaryl, or C 1 to C 3 alkylheteroaryl; R. sub.4 is cyano, trifluoromethyl,--COR 9,--CO 2 R 9,--CONR 9 R 10,--OR 9,--SO 2 NR. sub.9 R 10, or--S(O) q R. sub.9 ; R. sub.9 and R 10 are each independently hydrogen, C 1 to C 8 alkyl, C 1 to C 3 alkylaryl, aryl, or R 9 and R 10 may together be taken to form a three-to seven-membered alkyl ring or a three-to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C 1 to C 3 alkyl; R 11 is hydrogen,--OR 12, or--NHCOR. sub.12 ; R. sub.12 is hydrogen, C 1 to C 6 alkyl, aryl, or C 1 to C 3 alkylaryl; q is 0, 1, or 2; a first chiral carbon is designated by an asterisk; a second chiral carbon is designated by #; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C 1 to C 4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C 1 to C 4 alkoxy, and the pharmaceutically acceptable salts thereof.These compounds are useful in treating migraine and other disorders are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT 1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

METHODOLOGY FOR THE FACILE AND REGIO-CONTROLLED SYNTHESIS OF INDOLES

A method based on organodimetallic reagents is described for the regiocontrolled synthesis of indoles which proceeds, generally, in one to two operations from commercially or readily available reactants.The method is applied to the synthesis of indole itself, 2-substituted, 3-substituted, 2,3-disubstituted and 6-substituatd indoles.