74173-87-8Relevant academic research and scientific papers
Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors
Ichikawa, Masanori,Yokomizo, Aki,Itoh, Masao,Sugita, Kazuyuki,Usui, Hiroyuki,Shimizu, Hironari,Suzuki, Makoto,Terayama, Koji,Kanda, Akira
scheme or table, p. 1930 - 1949 (2011/05/03)
To obtain small and efficient squalene synthase inhibitors, a flexible 2-aminobenzhydrol open form structure was designed and showed potent inhibitory activity comparable to 4,1-benzoxazepin compounds. Further chemical modification led to the discovery of a novel template with a strong squalene synthase inhibitory activity, and its basic structure-activity relationship was revealed. The X-ray crystallographic data of compound 12 bound to the active site of squalene synthase provided an important insight into the binding mode of this alternative template that formed 11-membered ring conformations with an intramolecular hydrogen bond.
An enantiopure galactose oxidase model: synthesis of chiral amino alcohols through oxidative kinetic resolution catalyzed by a chiral copper complex
Mannam, Sreedevi,Sekar, Govindasamy
experimental part, p. 497 - 502 (2009/07/18)
An enantiopure galactose oxidase (GO) enzyme model has been synthesized from readily available (R)-BINAM and Cu(OTf)2, and the enantiopure GO model has been effectively used in situ as an efficient chiral catalyst for the synthesis of chiral amino alcohols through oxidative kinetic resolution (OKR), where molecular oxygen is used as the sole oxidant. Under the proposed catalytic conditions, both ortho- and para-substituted amino alcohols were resolved with good to excellent enantiomeric excesses through oxidative kinetic resolution.
Synthesis of the antitumoural agent batracylin and related isoindolo[1,2-b]quinazolin-12(10H)-ones
Martínez-Viturro, Carlos M.,Domínguez, Domingo
, p. 1023 - 1026 (2008/02/04)
The synthesis of batracylin and related isoindolo[1,2-b]quinazolin-12-ones from easily accessible o-acylanilines is reported. The preparation of these tetracyclic compounds through a Mitsunobu reaction followed by spontaneous cyclodehydration shows the ability of this methodology to afford good yields of a wide variety of diversely 7, 8, 9, 10-substituted isoindoloquinazolinones in two steps.
Triazolo benzazepines
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, (2008/06/13)
There are presented benzazepines of the formula STR1 wherein either R1 is hydrogen, lower alkyl, 4-pyridyl or the group --(CH2)n --NR6 R7 and R2 and R3 together are an additional bond or R1 and R2 together are the oxo group and R3 is hydrogen or lower alkyl, R4 is phenyl, o-halophenyl or 2-pyridyl, R5 is halogen or nitro and either R6 is hydrogen or lower alkyl and R7 is hydrogen, lower alkyl, lower alkenyl or lower alkynyl or R6 and R7 together with the nitrogen atom are 4-(lower alkyl)-1-piperazinyl or 4-morpholinyl and n is the number 0 or 1, and their pharmaceutically acceptable acid additions salts. The compounds possess interesting psychotropic properties, i.e., pronounced anxiolytic properties have been established in the case of certain representative members of this class of substance.
2-[[2-Methyl-1-[2-benzoyl(or benzyl)phenyl]-1H-imidazol-5-yl]methyl]-1H-isoindole-1,3(2H)-diones
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, (2008/06/13)
A multistep process is presented for the preparation of imidazobenzodiazepines of the formula STR1 wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl. Also presented are novel intermediates utilized in the process. The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants. The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
