154985-93-0Relevant articles and documents
Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups
Jeffries, Benjamin,Wang, Zhong,Troup, Robert I.,Goupille, Ana?s,Le Questel, Jean-Yves,Fallan, Charlene,Scott, James S.,Chiarparin, Elisabetta,Graton, Jér?me,Linclau, Bruno
, p. 2141 - 2150 (2020)
A systematic comparison of lipophilicity modulations upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl substituents, at a single carbon atom, is provided using directly comparable, and easily accessible model compounds. In addition, comparison with relevant linear chain derivatives is provided, as well as lipophilicity changes occurring upon chain extension of acyclic precursors to give cyclopropyl containing compounds. For the compounds investigated, fluorination of the isopropyl substituent led to larger lipophilicity modulation compared to fluorination of the cyclopropyl substituent.
Preparation method of (1-fluorocyclopropyl) methylamine hydrochloride
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Paragraph 0026-0029; 0037-0075, (2020/06/17)
The invention provides a preparation method of (1-fluorocyclopropyl) methylamine hydrochloride, wherein (1-fluorocyclopropyl) methylamine hydrochloride is prepared by taking 1-fluorocyclopropane carboxylic acid as an initial raw material through the steps of reduction, ammoniation and the like. According to the method, the generation of fluoromethylation by-products in the preparation method in the prior art is avoided, the experimental operation is simple, the purity is high, the reaction yield is greatly improved compared with that of the existing method, the yield of the three-step reactioncan reach more than 60%, and the method is suitable for large-scale production.
3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
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Page/Page column 109, (2020/05/28)
Provided are cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor, compositions comprising said compounds, and uses of said compounds in the treatment or prevention of diseases in which M4 muscarinic acetylcholine receptors are involved, especially neurological and psychiatric disorders and diseases.
IMIDAZO[1,2-B]PYRIDAZINE IL-17A INHIBITORS
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Page/Page column 21; 54-55, (2020/07/25)
The invention provides certain difluorocyclohexyl-imidazopyridazinyl-imidazolidinone compounds of formula II as IL-17A inhibitors, pharmaceutical compositions thereof, and methods of using a compound of formula II to treat certain symptoms of psoriasis, rheumatoid arthritis or multiple sclerosis.
ACRYLIC ACID DERIVATIVE, PREPARATION METHOD AND USE IN MEDICINE THEREOF
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Paragraph 0085; 0086, (2018/10/11)
The present invention relates to an acrylic acid derivative as shown in general formula (I), a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, the preparation method thereof, a pharmaceutical composition containing same, and the use thereof as therapeutic agents, in particular as selective estrogen receptor degraders (SERD), wherein the substituents of general formula (I) are the same as those defined in the description.
Novel Compounds
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Paragraph 0750-0752, (2017/07/06)
The present specification provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an RORγ and/or RORγt mediated disease state.
BACE INHIBITORS
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Paragraph 0191; 0192, (2015/01/06)
The present invention provides a compound of Formula III: wherein A is: and Z, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof.
Intramolecular hydrogen bonding in (1-fluorocyclopropyl)methanol as studied by microwave spectroscopy and quantum chemical calculations
M?llendal,Leonov,De Meijere
, p. 163 - 169 (2007/10/03)
(1-Fluorocyclopropyl)methanol has been studied by microwave spectroscopy in the 12-61GHz spectral region. The rotational spectra of the ground and of four vibrationally excited states belonging to three different normal modes of one rotamer have been assi