869299-68-3Relevant academic research and scientific papers
Method for synthesizing trans-3-(3-chloro-2-fluoro-6-(1H-tetrazole-1-yl) phenyl) acrylic acid
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Paragraph 0062-0064, (2021/04/21)
The invention discloses a method for synthesizing trans-3-(3-chloro-2-fluoro-6-(1H-tetrazole-1-yl) phenyl) acrylic acid. The synthesis method sequentially comprises the following six steps: protecting amino by tert-butyloxycarbonyl, formylating, carrying
SUBSTITUTED OXOPYRIDINE DERIVATIVES
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Page/Page column 91, (2020/07/14)
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular vascular disorders, preferably thrombotic
ERBB/BTK INHIBITORS
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Page/Page column 98; 60, (2019/08/26)
Disclosed are compounds inhibiting ErbBs (e. g., EGFR or Her 2), especially mutant forms of ErbBs, and BTK, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compou
Teaching Old Compounds New Tricks: DDQ-Photocatalyzed C?H Amination of Arenes with Carbamates, Urea, and N-Heterocycles
Das, Somnath,Natarajan, Palani,K?nig, Burkhard
supporting information, p. 18161 - 18165 (2017/12/28)
The C?H amination of benzene derivatives was achieved using DDQ as photocatalyst and BocNH2 as the amine source under aerobic conditions and visible light irradiation. Electron-deficient and electron-rich benzenes react as substrates with moderate to good product yields. The amine scope of the reaction comprises Boc-amine, carbamates, pyrazoles, sulfonimides and urea. Preliminary mechanistic investigations indicate arene oxidation by the triplet of DDQ to radical cations with different electrophilicity and a charge transfer complex between the amine and DDQ as intermediate of the reaction.
PHARMACEUTICAL COMPOUND
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Page/Page column 37, (2017/04/11)
Provided is a compound having formula (I): wherein R2 is selected from -C1, -Br and -CN; R1 and R4 are independently selected from H and -F; R631, R632, R641 and R642
FACTOR XIa INHIBITORS
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Page/Page column 59, (2016/11/02)
The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS
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Paragraph 1983-1986, (2015/12/23)
The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR1 (R1 is a hydrogen atom or an optionally substituted hydrocarbon group), is a single bond or a double bond, R2 is a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X′ is S, O, SO, or CH2), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]2 hydroxypropyl}5,6 dimethyl 4 oxo 1,4 dihydrothieno[2,3-d]pyrimidine-2-carboxamide is excluded, or a salt thereof.
Outer-sphere direction in iridium C-H borylation
Roosen, Philipp C.,Kallepalli, Venkata A.,Chattopadhyay, Buddhadeb,Singleton, Daniel A.,Maleczka, Robert E.,Smith, Milton R.
supporting information; experimental part, p. 11350 - 11353 (2012/08/29)
The NHBoc group affords ortho selective C-H borylations in arenes and alkenes. Experimental and computational studies support an outer sphere mechanism where the N-H proton hydrogen bonds to a boryl ligand oxygen. The regioselectivities are unique and com
Robust synthesis of methyl 5-chloro-4-fluoro-1 h -indole-2-carboxylate: A key intermediate in the preparation of an HIV NNRTI candidate
Mayes, Benjamin A.,Chaudhuri, Narayan C.,Hencken, Christopher P.,Jeannot, Frederic,Latham, G. Mark,Mathieu, Steven,Mcgarry, F. Patrick,Stewart, Alistair J.,Wang, Jingyang,Moussa, Adel
experimental part, p. 1248 - 1253 (2011/04/18)
A synthetic preparation of methyl 5-chloro-4-fluoro-1H-indole-2- carboxylate, a key intermediate towards phosphoindole inhibitors of HIV non-nucleoside reverse transcriptase, is described. The five-step synthesis involved Boc protection of the commercially available 4-chloro-3-fluoroaniline and regioselective iodination at C-2. After facile Boc deprotection, cyclization of the resultant o-iodoaniline gave the corresponding 5-chloro-4-fluoro-indole- 2-carboxylic acid which was subsequently esterified to provide the target indole ester in 56% overall yield. Identification of 6-chloro-7-iodo-2(3H)- benzoxazolone as a significant side product in the iodination step led to the development of conditions which eliminated its formation in subsequent batches. Advantages of this alternative approach relative to existing methodologies include (1) potentially hazardous diazonium and azido species were not required, (2) regioisomeric products were not generated, and (3) chromatographic isolations were avoided, as all intermediates were easily crystallized. As a result, the key indole ester was produced rapidly at 100-fold increased scale compared to previous reports with a 10-fold improvement in overall yield.
Process for the preparation of an indole derivative
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Page/Page column 9, (2009/01/24)
A process for the preparation of indole derivatives of formula (I): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
