474711-11-0Relevant articles and documents
A study of enantioselective syntheses by Sharpless asymmetric oxidation for aryl sulfoxides containing oxygen groups at the ortho position
Takei, Takanori,Takayama, Jun,Xuan, Meiyan,Tomoda, Misa,Miyamae, Hiroshi,Sakamoto, Takeshi
, (2021/03/16)
Abstract: While ortho-alkoxy aryl sulfoxides including various substituents were synthesized by Sharpless asymmetric oxidation reaction, we optimized the reaction conditions and screened better combination of starting materials to obtain high enantioselectivity. The result suggested new information that electron-withdrawing substituents on the aromatic ring have a strong influence upon enantioselectivity of the products. Also, several chiral ligands for Sharpless asymmetric oxidation reaction were evaluated to improve the enantioselectivity. Graphic abstract: High enantioselectivity of ortho-alkoxy aryl chiral sulfoxides have been achieved by Sharpless oxidation reaction using Ti(O-i-Pr)4 and diethyl tartrate under anhydrous condition. In particular, the enantioselctivity of products was influenced by electron-withdrawing substituents on the aromatic ring, such as nitro, ester and aldehyde groups.[Figure not available: see fulltext.]
ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 78, (2021/05/21)
The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.
ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 62; 106-107, (2021/01/22)
The disclosure relates to compounds that act as an allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.
Rhodium(II)-Catalyzed Aryl C?H Carboxylation of 2-Pyridylphenols with CO2
Cai, Zhihua,Li, Shangda,Gao, Yuzhen,Li, Gang
supporting information, p. 4005 - 4011 (2018/09/20)
A protocol for C?H carboxylation of electron-deficient 2-pyridylphenols with CO2 through a Rh(II)-catalyzed C?H bond activation under redox-neutral conditions has been developed. A suitable phosphine ligand was crucial for this reaction. This m
CHIRAL DIARYL MACROCYCLES AS MODULATORS OF PROTEIN KINASES
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Paragraph 0450, (2017/01/23)
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
Bismuth trichloride–mediated cleavage of phenolic methoxymethyl ethers
Obaro-Best, Oghale,Reed, Jack,Norfadilah, Alya A. F. B.,Monahan, Ryan,Sunasee, Rajesh
supporting information, p. 586 - 593 (2016/06/08)
A simple and efficient method for removal of phenolic methoxymethyl ethers in the presence of 30?mol% of bismuth trichloride in acetonitrile/water is described. Notable features of the cleavage protocol entail use of an ecofriendly bismuth reagent, ease of handling, low cost, operational simplicity, and good functional group compatibility. A number of structurally varied phenolic methoxymethyl ethers were cleaved in good to excellent yields.
Prostamide receptor antagonists
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Page/Page column 7-8, (2011/02/17)
The present invention provides prostamide receptor antagonist compounds that may be represented by the general formula I wherein A, R1, R2, R3, R4 and R6 are as defined in the specification.
Development of a new practical synthesis of a 5-HT2C receptor agonist
Gontcharov, Alexander,Potoski, John,Khafizova, Gulnaz,Shaw, Chia-Cheng,Yu, Qing,Tadayon, Sam,Bernatchez, Michel,Lankau, Mark,Cantin, Michel,Stack, Gary,Gross, Jonathan,Zhou, Dahui
body text, p. 1438 - 1447 (2011/09/20)
A new practical synthesis of a 5-HT2C receptor agonist has been developed and implemented on multikilogram scale. The key step, the selective epoxide opening in the glycidyl tosylate with the aryl Grignard reagent, allowed the incorporation of this commercially available chiral C3 synthon into the molecule and elaboration of the resulting intermediate into the target aminomethyldihydrobenzofuran without loss of enantiomeric purity.
NOVEL PROSTAMIDE RECEPTOR ANTAGONISTS
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, (2008/06/13)
The present invention provides prostamide receptor antagonist compounds that may be represented by the general formula I. wherein A, R1, R2, R3, R4 and R6 are as defined in the specification.
2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS
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Page 65-66, (2008/06/13)
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.