- A stereocontrolled total synthesis of (±)-norzizanone
-
A stereocontrolled total synthesis of (±)-norzizanone 1 has been efficiently accomplished involving base-induced rearrangement of the mesylate 17 as the key step. Aryl participated intramolecular cyclisation of the bromophenol 11 provided the tricyclic dienone 12, which was stereoselectively converted into the mesylate 17. (C) 2000 Elsevier Science Ltd.
- Pati, Lokesh Chandra,Roy, Arnab,Mukherjee, Debabrata
-
-
Read Online
- FLUOROALLYLAMINE DERIVATIVE AND USE THEREOF
-
The present invention relates to a fluoroallylamine derivative and use thereof. In particular, the present invention relates to a compound as shown in Formula I, a prodrug, an isomer, an isotope-labeled compound, a solvate or a pharmaceutically acceptable salt thereof, which has VAP-1/SSAO inhibitory activity, and can be used for treating a disease associated with VAP-1/SSAO overactivity.
- -
-
Paragraph 0272
(2020/03/17)
-
- Gold(I)-Catalyzed Intramolecular C(sp3)?H Insertion by Decarbenation of Cycloheptatrienes
-
A novel synthesis of indanes and dihydronaphtalenes based on the intramolecular insertion into C(sp3)?H bonds of gold(I) carbenes generated by retro-Buchner reaction (decarbenation) has been developed. Deuterium-labeling and kinetic isotope effect experiments, DFT calculations, and generation of the proposed carbene intermediate from a well-characterized gold(I) carbenoid support the involvement of a three-center concerted mechanism for the C(sp3)?H functionalization process.
- Yin, Xiang,Zuccarello, Giuseppe,García-Morales, Cristina,Echavarren, Antonio M.
-
supporting information
(2019/05/29)
-
- Selective sp3 C-H bond activation based on a carbocation relay: Friedel-Crafts reaction with alkanes as the alkylating component
-
A highly efficient and selective intramolecular Friedel-Crafts reaction of 3-methylbutyl or 4-methylpentyl-substituted aromatics has been developed using a carbocation relay strategy through selective sp3 C-H bond activation, providing a facile and cost-effective approach for the construction of benzocyclic compounds. A variety of 1,1-dimethylindane and naphthalene derivatives have been prepared from very simple starting materials in good yields with high selectivity. The present strategy has provided a new example of a Friedel-Crafts reaction with alkanes as the alkylating component and constitutes a convenient approach to selective C-H bond activation and functionalization of alkane derivatives. A highly efficient and selective intramolecular Friedel-Crafts reaction of 3-methylbutyl or 4-methylpentyl- substituted aromatics has been developed using a carbocation relay strategy through selective sp3 C-H bond activation. The approach provides a facile and cost-effective route to benzocyclic compounds. Copyright
- Wang, Jie,Zhou, Pengfei,Wang, Yang
-
experimental part
p. 264 - 270
(2011/03/20)
-
- HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS
-
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
- -
-
Page/Page column 23-24
(2009/04/24)
-
- Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold
-
The lead optimization of a novel series of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. The chemical instability of the dihydro-benzo[a]carbazole lead 2 was successfully addressed in the design and eval
- Marsilje, Thomas H.,Alper, Phil B.,Lu, Wenshuo,Mutnick, Daniel,Michellys, Pierre-Yves,He, Yun,Karanewsky, Donald S.,Chow, Donald,Gerken, Andrea,Lao, Jianmin,Kim, Min-Ju,Seidel, H. Martin,Tian, Shin-Shay
-
scheme or table
p. 5259 - 5262
(2009/05/07)
-
- Compounds having activity as inhibitors of cytochrome P450RAI
-
Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
- -
-
Page column 64
(2010/01/31)
-
- Compounds having activity as inhibitors of cytochrome P450RAI
-
Compounds having Formula 2 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
- -
-
Page column 62
(2010/01/31)
-
- Compounds having activity as inhibitors of cytochrome P450RAI
-
Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
- -
-
Page column 30, 63
(2010/11/29)
-
- Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
-
Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
- -
-
-
- Compounds having activity as inhibitors of cytochrome P450RAI
-
Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
- -
-
-