71556-74-6Relevant articles and documents
Method for preparing MPTF-E (meptazinol E)
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, (2016/10/09)
The invention discloses a method for preparing MPTF-E (meptazinol E), and belongs to the technical field of chemical drug preparation. The method comprises the following steps: (1) chloroanisole reacts with N-methylcaprolactam, and a compound I is obtained; (2) the compound I reacts with iodoethane, and a compound II is obtained; (3) boron bromide reacts with the compound II, and a compound III is obtained; (4) the compound III reacts with bromobutane, and a compound IV is obtained; (5) the compound IV is dissolved in anhydrous THF (tetrahydrofuran), lithium aluminum hydride is added, reaction reflux is performed, reactants are cooled to the room temperature, H2O is slowly added to a reaction liquid, then MgSO4 is added for stirring, filtration, reduced-pressure distillation and purification are performed, and a compound V is obtained. The method has the following advantages that MPTF-E is synthesized for the first time, and qualified impurity E comparison products are provided for meptazinol; a reagent adopted is a common solvent and easy to obtain; safe solvents such as ethyl acetate, petroleum ether and the like are used for treatment and have low toxicity; the process is simple and easy to operate, little energy is consumed, the stability is high, and the purity is high.
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents
DeSolms, S. Jane,Ciccarone, Terrence M.,MacTough, Suzanne C.,Shaw, Anthony W.,Buser, Carolyn A.,Ellis-Hutchings, Michelle,Fernandes, Christine,Hamilton, Kelly A.,Huber, Hans E.,Kohl, Nancy E.,Lobell, Robert B.,Robinson, Ronald G.,Tsou, Nancy N.,Walsh, Eileen S.,Graham, Samuel L.,Beese, Lorena S.,Taylor, Jeffrey S.
, p. 2973 - 2984 (2007/10/03)
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.
2-Bromo-3-methoxycyclohex-2-enone, a New Reagent for the α-Arylation of Lactams
Shepherd, Robin G.,White, Alan C.
, p. 2153 - 2156 (2007/10/02)
We report efficient syntheses of 2-bromo and 2-chloro-3-methoxycyclohex-2-enone and their use as m-hydroxyphenyl cation synthons for the α-arylation of lactams.The sequence has been used to synthesize the analgesic drug meptazinol.