58551-83-0Relevant academic research and scientific papers
Preparation method of 2, 4, 6-trifluoromethylmethylamine (by machine translation)
-
Paragraph 0009; 0011; 0013, (2020/04/17)
2, 4, 6 - Trifluorobenzaldehyde, is reacted with hydrogen under the action of a nickel catalyst to obtain the crude, trifluoromethylmethanamine, and the crude product, is obtained by reaction with hydrogen under the action of a nickel 2, 4, 6 - catalyst t
Continuous synthetic method of 2,4,6-trifluorobenzaldehyde
-
Paragraph 0035-0082, (2019/11/13)
The invention discloses a continuous synthetic method of 2,4,6-trifluorobenzaldehyde. The continuous synthetic method comprises the following steps that 1,3,5-trifluorobenzene, n-butyl lithium and N,N-dimethylformamide are taken as raw materials, and a co
A 2, 4, 6- three fluorine animal pens method for the preparation of amine compounds
-
Paragraph 0030; 0031, (2017/01/23)
The invention relates to a preparation method of a 2,4,6-trifluoro-benzylamine compound. The preparation method comprises the following steps: taking 1,3,5-trifluoro-benzene as a raw material, and preparing 2,4,6-trifluoro-benzylamine through lithiation, formylation, reduction, halogenation and replacement reaction. The reaction condition is mild, the operability is high, the atom economy is high, the technology is simple and easy to realize industrialization, and the product is high in purity and stable in quality, so that the compound accords with the using requirement of being as an intermediate.
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs
Cantrell, Amanda S.,Engelhardt, Per,H?gberg, Marita,Jaskunas, S. Richard,Johansson, Nils Gunnar,Jordan, Christopher L.,Kangasmets?, Jussi,Kinnick, Michael D.,Lind, Peter,Morin Jr., John M.,Muesing,Noreén, Rolf,?berg, Bo,Pranc, Paul,Sahlberg, Christer,Ternansky, Robert J.,Vasileff, Robert T.,Vrang, Lotta,West, Sarah J.,Zhang, Hong
, p. 4261 - 4274 (2007/10/03)
Phenylethylthiazolylthiourea (PETT) derivatives have been identified as a new series of nonnucleoside inhibitors of HIV-1 RT. Structure-activity relationship studies of this class of compounds resulted in the identification of N-[2-(2-pyridyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea hydrochloride (trovirdine; LY300046.HCl) as a highly potent anti-HIV-1 agent. Trovirdine is currently in phase one clinical trials for potential use in the treatment of AIDS. Extension of these structure-activity relationship studies to identify additional compounds in this series with improved properties is ongoing. A part of this work is described here. Replacement of the two aromatic moleties of the PETT compounds by various substituted or unsubstituted heteroaromatic rings was investigated. In addition, the effects of multiple substitution in the phenyl ring were also studied. The antiviral activities were determined on wild-type and constructed mutants of HIV-1 RT and on wild-type HIV-1 and mutant viruses derived thereof, Ile100 and Cys181, in cell culture assays. Some selected compounds were determined on double- mutant viruses, HIV-1 (Ile100/Asn103) and HIV-1 (Ile100/Cys181). A number of highly potent analogs were synthesized. These compounds displayed IC50's against wild-type RT between 0.6 and 5 nM. In cell culture, these agents inhibited wild-type HIV-1 with ED50's between I and 5 nM in MT-4 cells. In addition, these derivatives inhibited mutant HIV-1 RT (Ile 100) with IC50's between 20 and 50 nM and mutant HIV-1 RT (Cys 181) with IC50's between 4 and 10 nM, and in cell culture they inhibited mutant HIV-1 (Ile100) with ED50's between 9 and 100 nM and mutant HIV-1 (Cys181) with ED50's between 3 and 20 nM.
