A facile synthesis of bicyclo[m.n.1]alkan-1-ols. Evidence for organosamarium intermediates in the samarium(II) iodide promoted intramolecular Barbier-type reaction
摘要:
Samarium(II) iodide (SmI2) has been successfully employed as a reductive coupling agent for the intramolecular Barbier-type synthesis of bicyclo[m.n.1]alkan-1-ols. Thus, a variety of 3-(omega-iodoalkyl)cycloalkanones, upon treatment with SmI2 and a catalytic quantity of iron complex in tetrahydrofuran (THF), provide the title compounds in excellent yields. The reaction is quite general for the construction of diverse bicyclic ring systems, including the highly strained bicyclo[2.1.1]hexan-1-ol. In addition to exploring the synthetic utility of this reaction, studies have been performed which provide insight on the mechanistic details of the SmI2-promoted intramolecular Barbier-type synthesis. Compelling evidence for the intermediacy of organosamarium species has thus been gathered.
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I):
wherein each symbol is as defined in the present specification, or a salt thereof.
METHOD FOR ASSAY ON THE EFFECT OF VASCULARIZATION INHIBITOR
申请人:Uenaka Toshimitsu
公开号:US20100092490A1
公开(公告)日:2010-04-15
The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
Migration aptitudes of cyclic and polycyclic bridgehead groups in the Criegee Rearrangement
作者:Eckehardt Wistuba、Christoph Rüchardt
DOI:10.1016/s0040-4039(01)81913-4
日期:1981.1
The migrationaptitudes of cyclic and polycyclic bridgehead groups in the Criegee Rearrangement support σ-neighbouring group participation by pentacoordinated bonding and vertical charge stabilisation in the migrating group and therefore favour transition state 2b and not 2a.
FUSED TRIAZOLES FOR THE TREATMENT OR PROPHYLAXIS OF MILD COGNITIVE IMPAIRMENT
申请人:Koike Tatsuki
公开号:US20130178497A1
公开(公告)日:2013-07-11
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
Antibacterial solid composition for oral administation
申请人:Takeda Chemical Industries, Ltd.
公开号:EP0163433A2
公开(公告)日:1985-12-04
This invention relates to an antibacterial solid composition for oral administration which comprises a lipid soluble cephalosporin compound and a cyclodextrin. The said composition provides much increased in vivo absorbability of a non-ester form of the cephalosporin compound. This composition is useful for prevention and treatment of bacterial infections.