188359-85-5Relevant articles and documents
A west he row sandbank intermediate preparation method
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Paragraph 0065; 0066; 0069; 0078; 0086, (2017/08/25)
The invention discloses a preparation method for a sitagliptin intermediate and belongs to the field of drug synthesis. The preparation method comprises the following steps: (1) carrying out a ring-opening reaction: carrying out Grignard reaction on 2,4,5-trifluorobromobenzene and a Grignard reagent RMgX in a medium of tetrahydrofuran and methyl tertiary-butyl ether at (-20) DEG C to 50 DEG C by taking cuprous chloride as a catalyst, wherein R2 is isopropyl and X is halogen, and then carrying out the ring-opening reaction on the generated compound and a compound shown in a formula 3 to obtain a compound shown in a formula 4; and (2) carrying out an oxidizing reaction: carrying out the oxidizing reaction on the compound shown in the formula 4 and potassium permanganate in an acetone medium, quenching and neutralizing the product by using reducing agents sodium sulfite and sodium hydrogen sulfite, and extracting the product by methyl tertiary butyl ether to obtain the sitagliptin intermediate. The method is low in cost, high in yield, mature in process and suitable for industrial production.
QUINOLYL PYRROLO PYRIMIDYL CONDENSED-RING COMPOUND AND SALT THEREOF
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Paragraph 0328-0330; 0335-0337, (2014/03/24)
The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based o
Exploring Leishmania major Inositol Phosphorylceramide Synthase (LmjIPCS): Insights into the ceramide binding domain
Mina, John G.,Mosely, Jackie A.,Ali, Hayder Z.,Denny, Paul W.,Steel, Patrick G.
supporting information; experimental part, p. 1823 - 1830 (2011/04/26)
The synthesis of set of ceramide analogues exploring hydrophobicity in the acyl chains and the degree and nature of hydroxylation is described. These have been assayed against the parasitic protozoan enzyme LmjIPCS. These studies showed that whilst the C-3 hydroxyl group was not essential for turnover it provided enhanced affinity. Reflecting the membrane bound nature of the enzyme a long (C13) hydrocarbon ceramide tail was necessary for both high affinity and turnover. Whilst the N-acyl chain also contributed to affinity, analogues lacking the amide linkage functioned as competitive inhibitors in both enzyme and cell-based assays. A model that accounts for this observation is proposed.
NOVEL COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ GAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASE
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Page/Page column 57; 58, (2011/10/03)
The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administrating these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
Chiral electrophilic 'glycinal' equivalents. New synthons for optically active α-amino acids and 4-substituted 2-oxazolidinones
Matsunaga, Hirofumi,Ishizuka, Tadao,Kunieda, Takehisa
, p. 1275 - 1294 (2007/10/03)
The thermal reaction of 3-[(1S)-2-alkoxy-1-apocamphanecarbonyl]-2-oxazolones (21a-c) with dialkyl azodicarboxylates (9) results in exclusive formation of [4 + 2] type cycloadducts (22 and 23) with moderate levels of diastereofacial selection (up to 72% d.e.). The diastereomers thus obtained were readily purified and subsequent treatment with acidic methanol followed by removal of the auxiliary with LiBH4/MeOH (1:2) gave optically pure 4-methoxy-5-hydrazino-2-oxazolidinones (26 and 27), which serve as α-aminoaldehyde templates useful for the synthesis of a wide variety of optically active α-amino acids as well as 4-alkyl and 4-aryl-2-oxazolidinones.