摘要:
A direct trifluoromethylation method preferably using a trifluoromethane as a fluoromethylating species. In particular, the present method is used for preparing a trifluoromethylated substrate by reacting a fluoromethylatable substrate with a trifluoromethylating agent in the presence of an alkoxide or metal salt of silazane under conditions sufficient to trifluoromethylate the substrate; wherein the fluoromethylatable substrate includes chlorosilanes, carbonyl compounds such as esters, aryl halides, aldehydes, ketones, chalcones, alkyl formates, alkyl halides, aryl halides, alkyl borates, carbon dioxide or sulfur.
摘要:
The present invention relates to the treatment of tuberculosis (mycobacterial infections) by the use of KshAB complex inhibitors, or a KstD molecule, or a HsaAB complex, or a HsaC molecule, or a HsaD molecule. The application also includes a method for identifying an inhibitor or modulator of the previously mentioned molecules and complexes.
摘要:
Die vorliegende Erfindung betrifft ein Verfahren zur kontinuierlichen Herstellung von 2-Brom-2-nitro-1, 3-propandiol, bei dem man I) Nitromethan und eine oder zwei wässrige Lösungen, enthaltend Formaldehyd und Alkalihydroxid unter Durchmischung kontinuierlich einer ersten, gekühlten Reaktionszone mit Molverhältnissen von Formaldehyd zu Nitromethan im Bereich von 1,9 bis 2,2:1 und Alkalihydroxid zu Nitromethan im Bereich von 0,95:1 bis 1,1:1 zuführt, II) die in I) erhaltene wässrige Reaktionsmischung kontinuierlich der ersten Reaktionszone entnimmt und diese direkt im Anschluss daran zusammen mit Brom wenigstens einer zweiten, gekühlten Reaktionszone kontinuierlich zuführt, und III) 2-Brom-2-nitro-1,3-propandiol aus der in II) erhaltenen wässrigen Reaktionsmischung isoliert.
摘要:
Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula (I), as defined further herein.
摘要:
A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]-amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipemia and so on; and intermediates therefor as represented by general formula (5) or (6) or the like wherein R is hydrogen or the like; B is chloro or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3- nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.
摘要:
Compounds of formula (I), wherein R is an aromatic or a heteroaromatic ring; R and R are H, C1-C8alkyl, aryl, arylC1-C8alkyl, or heteroaryl; R is an aromatic or a heteroaromatic ring or an amine; W, X, Y, are independently selected from the group consisting of CH, N, S, or O, provided that at least one of W, X, and Y is a heteroatom, which inhibit protease, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease therewith.
摘要翻译:式(I)的化合物,其中R 1是芳族或杂芳族环; R 2和R 3是H,C 1 -C 8烷基,芳基,芳基C 1 -C 8烷基或杂芳基; R 4是芳族或杂芳环或胺; W,X,Y独立地选自CH,N,S或O,条件是W,X和Y中的至少一个是杂原子,其抑制蛋白酶,包括组织蛋白酶K,药物组合物 这些化合物和用于治疗过度骨丢失或软骨或基质降解(包括骨质疏松症)的疾病的方法; 牙龈疾病包括牙龈炎和牙周炎; 关节炎,骨关节炎和类风湿性关节炎; 佩吉特病 恶性高钙血症; 和代谢性骨病。
摘要:
The present invention provides the processes for the preparation of eltrombopag of Formula (I) or its pharmaceutically acceptable salts. The invention also provides crystalline forms of eltrombopag.
摘要:
The present invention provides the processes for the preparation of eltrombopag of Formula (I) or its pharmaceutically acceptable salts. The invention also provides crystalline forms of eltrombopag.