255893-57-3Relevant articles and documents
The development of a practical synthesis of the potent and selective somatostatin sst3 receptor antagonist [4-(3,4-difluoro-phenyl)- piperazine-1-yl]-{(4S,4aS,8aR)-2[(S)-3-(6-methoxy-pyridin-3-yl)-2-methyl-propyl] -decahydroisoquinoline-4-yl}-methanone (NVP-ACQ090)
Baenziger, Markus,Cercus, Jacques,Hirt, Hans,Laumen, Kurt,Malan, Christophe,Spindler, Felix,Struber, Fritz,Troxler, Thomas
, p. 3469 - 3477 (2003)
The decahydroisoquinoline derivative NVP-ACQ090 is a potent and selective antagonist at the somatostatin sst3 receptor. The original research synthesis of NVP-ACQ090 comprises a main chain of nine linear steps and two side chains of three and steps, respectively. This synthesis is highly convergent, but very complex and expensive, and involves several reagents that are not acceptable for a large scale synthesis. In chemical development, all the unacceptables could be replaced, and the overall efficiency of the synthesis was much improved.
Microwave-assisted amination from fluorobenzenes without catalyst and strong base
Meng, Xiangguo,Cai, Zhengyan,Xiao, Sa,Zhou, Weicheng
, p. 70 - 75 (2013/03/14)
A facile and versatile amination of fluorobenzenes has been developed in good to excellent yields under microwave irradiation in N-methylpyrrolidinone (NMP) without strong base and catalyst. The presence of additional halogen atom(s) enhanced the leaving ability of fluorine and meta fluorine gave higher activation than the ortho. It is remarkable that 1,2,3-trifluorobenzene, 1,2,4-trifluorobenzene and 1,2,4,5-tetrafluorobenzene can produce the regioselective mono-substituted products.
SUBSTITUTED DIHYDROCHINAZOLINES HAVING ANTIVIRAL PROPERTIES
-
Page/Page column 31, (2008/06/13)
The invention relates to substituted dihydrochinazolines of formula (I), methods for the production thereof, and the use thereof for producing medicaments used for treating and/or preventing diseases, particularly as antiviral agents, especially against cytomegaloviruses.