129306-07-6Relevant academic research and scientific papers
A 5-benzyl -7 (S)-tert-butoxycarbonylamino-5-azaspiro [2,4] heptane preparation method of
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, (2017/01/23)
The invention discloses a preparation method for 5-benzyl-7(S)-t-butyloxycarborylamino-5-aza-spiro[2,4]heptane. The method comprises the following steps: reacting benzoylamide acetoacetate as a raw material with 1,2-dichloroethane to obtain 3-cyclopropyl benzoylamide acetoacetate, brominating 3-cyclopropyl benzoylamide acetoacetate by NBS (n-bromosuccinimide) to obtain 1-bromo-3-cyclopropyl benzoylamide acetoacetate, cyclizing under alkaline conditions to obtain 5-benzyl-5-aza-spiro[2,4]heptane-4,7-diketone, further reacting with hydroxylamine hydrochloride to form an oxime compound-4-oxo-5-benzyl-7-oximido-5-aza-spiro[2,4]heptane, reducing by NaBH4 and boron trifluoride diethyl etherate to obtain 5-benzyl-7-amino-5-aza-spiro[2,4]heptane, performing chiral resolution by a resolving agent-L-camphorsulfonic acid to obtain 5-benzyl-7(S)-amino-5-aza-spiro[2,4]heptane, and reacting with di-tert-butyl dicarbonate ester to obtain 5-benzyl-7(S)-t-butyloxycarborylamino-5-aza-spiro[2,4]heptane. According to the method, an intermediate body-carbonyl does not need protection, raw materials are easy to get, a process route is simple, and the method is suitable for industrial production.
Substituted alkynyl pyridine compounds and methods of use thereof, and use thereof
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, (2016/10/08)
The invention provides a substituted alkynylpyridine compound with a structure represented by a formula (I) as described in the specification and a pharmaceutically acceptable salt and a medicinal preparation thereof. The compound is used for adjusting activity of protein kinase and adjusting intercellular or intracellular signal response. The invention also relates to a pharmaceutical composition including the compound provided by the invention and a method of applying the pharmaceutical composition in treating mammals, especially in treating highly proliferative diseases of the mankind.
SUBSTITUTED ALKYNYL PYRIDINE COMPOUNDS AND METHODS OF USE
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, (2014/01/07)
The present invention provides novel substituted alkynyl pyridine compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
PEPTIDE DEFORMYLASE INHIBITORS
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Page/Page column 178, (2009/06/27)
The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I), wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
Synthesis and In-Vitro Activity of Novel 1β-Methylcarbapenems Having Spiro[2,4]heptane Moieties
Park, Hyeong Beom,Jo, Nam Hyun,Hong, Joon Hee,Chei, Jung Hoon,Cho, Jung-Hyuck,Yoo, Kyung Ho,Oh, Chang-Hyun
, p. 530 - 537 (2008/12/21)
The synthesis of a new series of 1β-methylcarbapenems having spiro[2,4]heptane moieties is described. Their in-vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. Most compounds were shown to be more active than the compared meropenem and imipenem against Escherichia coli. One particular compound, IIIb, having hydroxy a moiety showed the most potent antibacterial activity.
