357670-16-7

Usage

Uses

Used in Pharmaceutical Industry:
Ethyl 1-(2-cyanophenyl)piperidine-4-carboxylate is used as a key intermediate in the synthesis of PDE V inhibitors for the development of medications targeting erectile dysfunction, pulmonary arterial hypertension, and other related conditions. Its unique structure allows for the creation of effective and selective PDE V inhibitors, which can improve blood flow and treat the mentioned disorders.

Upstream product

• 1126-09-6 4-carbethoxypiperidine 
• 394-47-8 2-fluorobenzonitrile 

Downstream Products

• 220060-39-9 3-ethyl-1,3-dihydro-8-[[[2-[4-(hydroxymethyl)-1-piperidinyl]phenyl]methyl]amino]-2H-imidazo[4,5-g]quinazoline-2-thione 
• 220060-79-7 2-[4-(hydroxymethyl)piperidino]benzylamine 

Relevant academic research and scientific papers

PHENYL mTORC INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

1, 4-DISUBSTITUTED PIPERIDINES AS VASOPRESSIN RECEPTOR VIA ANTAGONISTS

The present invention provides compounds of formula (1) compositions comprising such compounds; the use of such compounds in therapy (such as in the treatment of dysmenorrhoea); and methods of treating patients with such compounds; wherein A and G are as defined herein.

Method of inhibiting neoplastic cells with imidazoquinazoline derivatives

A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to imidazoquinazoline derivatives.

Development of a practical synthetic route of a PDE V inhibitor KF31327

An efficient route suitable for a large-scale preparation of KF31327 (1), a potent phosphodiesterase V inhibitor, has been developed. We selected 7-chloro-2,4(1H,3H)-quinazolinedione (15) as a starting material, which gave the desired 6-nitro compound with good selectivity. In the chlorination of 7-ethyl-amino-6-nitro-2,4(1H,3H)-quinazolinedione (17), reaction conditions were optimized to minimize the amount of phosphorus oxychloride, and 2,4-dichloro-7-ethylamino-6-nitroquinazoline (14) was obtained in excellent yield. After the selective substitution at C4 position, the chloro substituent at C2 position was successfully removed by hydrogenation concomitant with the reduction of nitro group. The construction of the imidazothione ring was achieved by using phenyl isothiocyanate as a thiocarbonyl donor instead of extremely flammable carbon disulfide. Multikilograms of drug substance have been successfully prepared by these procedures.

Imidazoquinazoline derivatives

PCT No. PCT/JP97/03023 Sec. 371 Date Apr. 27, 1998 Sec. 102(e) Date Apr. 27, 1998 PCT Filed Aug. 29, 1997 PCT Pub. No. WO98/08848 PCT Pub. Date Mar. 5, 1998Imidazoquinoline derivatives of the formula (wherein X may be O or S) provide selective cyclic guanosine 3',5' monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitory activity. The compounds are useful for treating or ameliorating cardiovascular disease such as thrombosis, angina pectoris, hypertension, heart failure and arterial sclerosis, as well as asthma, impotence and the like.