An approach to erythronolide A seco acid via a simple tetronic acid
摘要:
The unsaturated aldehyde 1, a key intermediate in our approach to erythronolide A seco acid (2), has been prepared from the simple tetronic acid 6 by its seriatim transformations into the vinylogous urethanes 5, 9, and 11 concluding with reductive conversion of the latter into 1.
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
PROCESS FOR PRODUCING OPTICALLY ACTIVE 4-CHLORO-3-HYDROXYBUTANAL COMPOUND
申请人:Hayashi Yujiro
公开号:US20130217901A1
公开(公告)日:2013-08-22
The invention relates to a method of producing optically active 4-chloro-3-hydroxybutanal compound (2) by reacting chloroacetaldehyde with aldehyde compound (1) in the presence of optically active pyrrolidine compound (5).
wherein each symbol is as defined in the specification.
The invention relates to new pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system and cancers. This invention also relates to pharmaceutical compositions containing these compounds.
Binaphthyl-based chiral ligands: design, synthesis and evaluation of their performance in enantioselective addition of diethylzinc to aromatic aldehydes
作者:Chao Yao、Piao Wu、Yue Huang、Yaoqi Chen、Lin Li、Yue-Ming Li
DOI:10.1039/d0ob02127j
日期:——
the performance of binaphthyl-based chiral ligands were evaluated with computation and enantioselective addition of diethylzinc to aromatic aldehydes. Under optimized conditions, enantioselective addition of diethylzinc to aromatic aldehydes provided the desired optically active secondary alcohols in high isolated yields (up to 91%) and excellent enantiomericexcesses (up to 98% ee).
A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided.
A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt:
[in the formula, X represents a carbon atom or a nitrogen atom;
X
1
, X
2
, X
3
and X
4
each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II):
(in the formula, X represents a carbon atom or a nitrogen atom); R
1
represents an aryl, etc.; R
2
represents a hydroxy, etc.; R
3
represents a —C
1-6
alkyl, etc.; R
4
represents a —C
1-6
alkyl, etc.; X
5
represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].