71556-71-3

Upstream product

• 768-66-1 2,2,6,6-tetramethyl-piperidine 
• 766-51-8 2-Chloroanisole 
• 3553-94-4 1-trimethylsilanyl-azepan-2-one 
• 77-78-1 dimethyl sulfate 
• 71556-81-5 3-(3-hydroxyphenyl)hexahydro-2H-azepin-2-one 
• 38227-87-1 2,2,6,6-tetramethylpiperidinyl-lithium 
• 105-60-2 caprolactam 

Downstream Products

• 71556-83-7 3-Ethylhexahydro-3-(3-methoxyphenyl)-2H-azepin-2-one 
• 71592-43-3 hexahydro-3-(3-methoxyphenyl)-1-methyl-2H-azepin-2-one 
• 275806-03-6 2-[3-(3-ethyl-azepan-3-yl)-phenoxy]-4-imidazol-1-ylmethyl-benzonitrile 
• 275807-69-7 3-ethyl-3-(3-hydroxy-phenyl)-azepan-2-one 
• 27180-90-1 3-ethyl-3-(3-methoxyphenyl)azepane 
• 59263-75-1 3-(3-ethylhexahydro<1H>azepine-3-yl)phenol 
• 71556-81-5 3-(3-hydroxyphenyl)hexahydro-2H-azepin-2-one 

Relevant academic research and scientific papers

Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents

A series of novel diaryl ether lactams have been identified as very potent dual inhibitors of protein farnesyltransferase (FTase) and protein geranylgeranyltransferase I (GGTase-I), enzymes involved in the prenylation of Ras. The structure of the complex formed between one of these compounds and FTase has been determined by X-ray crystallography. These compounds are the first reported to inhibit the prenylation of the important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to achieve this endpoint were rapidly lethal.

Inhibitors of prenyl-protein transferase

The present invention is directed to compounds which inhibit prenyl-protein transferase and particularly, the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this in

Inhibitors of prenyl-protein transferase

The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Process for preparing hexahydroazepine, piperidine and pyrrolidine derivatives

2-Oxo-hexahydroazepine, -piperidine or pyrrolidines of formula STR1 wherein n is 2,3 or 4, R is hydrogen, lower alkyl, aryl(lower)alkyl, loweralkenylmethyl or cycloalkylmethyl, R1 is hydrogen or lower alkyl and R2 is hydrogen, lower alkyl or aryl(lower)alkyl are prepared by a novel process involving reaction of an anion of a lactam of formula STR2 where R3 is lower alkyl, aryl(lower)alkyl, trialkyl-, triaryl- or triarylalkyl-silyl with a benzyne of formula STR3 where R4 is lower alkyl, aryl(lower)alkyl or trialkyl-, triaryl- or triarylalkyl-silyl. The products are useful as intermediates for preparing pharmacologically active 2-unsubstituted -hexahydroazepine, -piperidine and pyrrolidine derivatives.

Hexahydroazepine, piperidine and pyrrolidine derivatives

The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) STR1 where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R2 is hydrogen, lower alkyl or aryl(lower)alkyl and R3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.