4-Dodecylbenzenesulfonic acid (DBSA) promoted solvent-free diversity-oriented synthesis of primary carbamates, S-thiocarbamates and ureas
作者:Ali Reza Sardarian、Iman Dindarloo Inaloo
DOI:10.1039/c5ra14528g
日期:——
A simple and efficient solvent-free preparation of primary carbamates,S-thiocarbamates and ureas from alcohols, phenols, thiols and amines in the presence of 4-dodecylbenzenesulfonic acid, as a cheap and green Brønsted acid, has been described.
This invention relates to compounds of the formula:
wherein R is an electron withdrawing group;
R₁ is H or COZ;
X₁ and X₂ are independently H, lower alkyl, aryl, aryl lower-alkyl or polystyrene or
R and X₁ taken together with the carbon atoms to which they are attached form a ring containing from 4 to 15 ring carbon atoms and may contain up to 2 heteroatoms, wherein the heteroatoms are O, S, or N; and
Z is an amino acid residue, a peptide residue or a leaving group. The compounds of the present invention are adaptable as blocking or protecting groups for an amine composition useful in peptide synthesis. The present invention is also directed to a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.
本发明涉及式中的化合物:
其中 R 是取电子基团;
R₁ 是 H 或 COZ;
X₁ 和 X₂ 独立地为 H、低级烷基、芳基、芳基低级烷基或聚苯乙烯,或
R 和 X₁ 与它们所连接的碳原子一起形成一个环,该环含 4 至 15 个环状碳原子,最多可包含 2 个杂原子,其中杂原子为 O、S 或 N;以及
Z 是氨基酸残基、肽残基或离去基团。本发明的化合物可用作肽合成中胺类组合物的封端或保护基团。本发明还涉及一种在反应过程中保护有机分子氨基的方法,该反应改变了分子中除受保护氨基以外的部分。
Pyrrolotriazole derivative
申请人:FUJI PHOTO FILM CO., LTD.
公开号:EP0518238A1
公开(公告)日:1992-12-16
A novel pyrrolotriazole derivative is disclosed, represented by any one of formulae (I), (II), or (III):
wherein:
R¹, R², R³ and R⁴ each independently represents a hydrogen atom or a nonmetallic atomic group;
R⁵ and R⁶ each independently represents a hydrogen atom, alkyl group, an aryl group, or a heterocyclic group;
R⁷ represents an electrophilic group having a Hammett's substituent constant σp of 0.15 or more;
R⁸ and R⁹ each independently represents a hydrogen atom or a nonmetallic atomic group;
the sum of Hammett's substituent constant σp of R⁷ and R⁸ is 0.65 or more;
R¹ and R², and/or R² and R⁵, and/or R⁵ and R⁶, and/or R⁶ and R³, and/or R³ and R⁴ may be connected to each other to form a cyclic structure;
R⁷ and R⁸ may be connected to each other to form a cyclic structure; and
Z represents a hydrogen atom, a halogen atom, an arylthio group, a heterocyclic thio group, an arylsulfinyl group, or a nitroso group.
Imidazole azo dyes and thermal transfer dye donating materials containing them
申请人:FUJI PHOTO FILM CO., LTD.
公开号:EP0545420A2
公开(公告)日:1993-06-09
Disclosed is an imidazole azo dye of formula (I), which is useful for image formation and as a filter dye, which has a sharp absorption wave and which is fast to light, heat, air, moisture and chemicals. Also disclosed is a thermal transfer dye-donating material containing imidazole azo dye(s) of formula (I) preferably along with aminopyrazole azo dye(s) of formula (II). The material gives a high-density image with good color reproduction, and the image formed has improved storage stability.
In (I), B and C independently represent a hydrogen atom or a substituent capable of being substituted in the imidazole ring; A represents an aryl or heterocyclic group; provided that when B is a hydrogen atom, C is not a hydrogen atom nor an alkyl group having from 1 to 3 carbon atoms; provided that when C is a hydrogen atom, B is not a substituted nor unsubstituted alkyl group; provided that C is not a mercapto group or an alkylthio group; and provided that B is not a carboxyl group.
In (II), D represents a hydrogen atom, or an alkyl, aryl, or heterocyclic group, E represents a substituent capable of being substituted in the pyrazole ring, F represents an aryl or heteroaromatic group, and G and I independently represent a hydrogen atom, or an alkyl, aryl, or heterocyclic group.
本发明公开了一种式(I)的咪唑偶氮染料,该染料可用于形成图像和用作过滤染料,它具有尖锐的吸收波,并且对光、热、空气、湿气和化学品具有快速吸收性。本发明还公开了一种热转印染料捐赠材料,该材料最好含有式(I)的咪唑偶氮染料和式(II)的氨基吡唑偶氮染料。该材料可产生色彩再现性良好的高密度图像,所形成的图像具有更好的储存稳定性。
在(I)中,B 和 C 独立地代表氢原子或咪唑环中能够被取代的取代基;A 代表芳基或杂环基;条件是当 B 是氢原子时,C 不是氢原子或具有 1 至 3 个碳原子的烷基;条件是当 C 是氢原子时,B 不是取代或未取代的烷基;条件是 C 不是巯基或烷硫基;以及条件是 B 不是羧基。
在(II)中,D 代表氢原子或烷基、芳基或杂环基,E 代表吡唑环中可被取代的取代基,F 代表芳基或杂芳基,G 和 I 独立地代表氢原子或烷基、芳基或杂环基。
Carboline derivatives useful in the inhibition of angiogenesis
申请人:PTC Therapeutics, Inc.
公开号:EP2431369A2
公开(公告)日:2012-03-21
In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.