206446-39-1Relevant articles and documents
Synthetic method of antitumor heterocyclic drug intermediate 2-(3-azacyclobutyl) pyridine dihydrochloride
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Paragraph 0039; 0040, (2017/08/31)
The invention discloses a synthetic method of an antitumor heterocyclic drug intermediate 2-(3-azacyclobutyl) pyridine dihydrochloride. The synthetic method specifically comprises the following step of performing a two-step reaction to obtain a target compound 2-(3-azacyclobutyl) pyridine dihydrochloride by taking 3-iodine-1-t-butyloxycarboryl azetidine and 2-bromopyridine as raw materials. According to the synthetic method disclosed by the invention, the used raw materials are simple, low in cost and easily available, the reaction condition is simple, and the obtained product is high in chemical purity.
Continuous synthesis of organozinc halides coupled to Negishi reactions
Alonso, Nerea,Miller, L. Zane,De M. Muoz, Juan,Alczar, Jesus,McQuade, D. Tyler
supporting information, p. 3737 - 3741 (2015/01/16)
The Negishi cross-coupling is a powerful C-C bond forming reaction. The method is less commonly used relative to other cross-coupling methods in part due to lack of availability of organozinc species. While organozinc species can be prepared, problems wit
Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
Takhi, Mohamed,Sreenivas, Kandepu,Reddy, Chandrashekar K.,Munikumar, Mahadari,Praveena, Kolakota,Sudheer, Pabolu,Rao, Bandaru N.V.M.,Ramakanth, Gollamudi,Sivaranjani, Jampala,Mulik, Shardaprasad,Reddy, Yeruva R.,Narasimha Rao, Krishnamurthy,Pallavi, Rentala,Lakshminarasimhan, Anirudha,Panigrahi, Sunil K.,Antony, Thomas,Abdullah, Iskandar,Lee, Yean K.,Ramachandra, Murali,Yusof, Rohana,Rahman, Noorsaadah A.,Subramanya, Hosahalli
, p. 382 - 394 (2014/08/05)
A novel and potent series of ene-amides featuring azetidines has been developed as FabI inhibitors active against drug resistant Gram-positive pathogens particularly staphylococcal organisms. Most of the compounds from the series possessed excellent biochemical inhibition of Staphylococcus aureus FabI enzyme and whole cell activity against clinically relevant MRSA, MSSA and MRSE organisms which are responsible for significant morbidity and mortality in community as well as hospital settings. The binding mode of one of the leads, AEA16, in Escherichia coli FabI enzyme was determined unambiguously using X-ray crystallography. The lead compounds displayed good metabolic stability in mice liver microsomes and pharmacokinetic profile in mice. The in vivo efficacy of lead AEA16 has been demonstrated in a lethal murine systemic infection model.
AMINO-HETEROCYCLIC COMPOUNDS
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Page/Page column 30, (2010/08/07)
The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
Synthesis of C-substituted cyclic amines using azacycloalkyl organozinc reagents
Billotte
, p. 379 - 380 (2007/10/03)
Azetidine and piperidine derived organozinc species have been prepared from the corresponding azacycloalkyl iodides by direct Zn insertion. They have been shown to readily undergo Pd(0) mediated cross-coupling reactions and to transmetallate with CuCN.2LiCl.