- A METHOD FOR THE PREPARATION OF FINGOLIMOD
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The invention relates to a method of preparation of 2-amino-2-[2-(4-octylphenyl)- ethyl]propane-1,3-diol (I), comprising opening of the aziridine ring of the intermediates (LVI) by the treatment with organometallic compounds, preferably the Grignard reage
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- A convenient synthesis of the immunosuppressive agent FTY720
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This paper describes a practical synthetic approach to preparation of an immunosuppressant, FTY720. The key steps involve an iron-catalyzed cross-coupling reaction and a Wittig reaction. The advantages of this synthesis include readily available starting
- Feng, Xiangjun,Mei, Yuhua,Luo, Yu,Lu, Wei
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experimental part
p. 161 - 164
(2012/07/03)
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- S1P RECEPTORS MODULATORS AND THEIR USE THEREOF
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The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.
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Page/Page column 51
(2010/04/30)
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- S1P RECEPTORS MODULATORS
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The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
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Page/Page column 88
(2010/04/30)
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- Odorless substitutes for foul-smelling thiols: Syntheses and applications
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Several alkanethiols and p-alkylphenylmethanethiols were synthesized, and their odors were compared with those of ethanethiol and benzyl mercaptan by human and instrumental sensors. Among the various thiols analyzed, 1-dodecanethiol (1) and p-heptylphenylmethanethiol (3) were revealed to be odorless. 1-Dodecanethiol (1) has been used instead of ethanethiol for dealkylation of ethers, and p-heptylphenylmethanethiol (3) can replace benzyl mercaptan in the preparation of a 1,3-mercapto alcohol from an α,β-unsaturated ketone. These odorless thiols will greatly improve the physical environment of the researcher working with these foul-smelling compounds.
- Node, Manabu,Kumar, Kamal,Nishide, Kiyoharu,Ohsugi, Shin-Ichi,Miyamoto, Tetsuo
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p. 9207 - 9210
(2007/10/03)
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- Enantioselective Extraction of Di-O-benzoyltartrate Anion by Ion-Pair Extractant Having Binaphthyl-Unit
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A lipophilic diphosphonium salt 1 having binaphthyl-type axial chirality was developed as a novel ion-pair extractant.By use of (R)-1, (-)-di-O-benzoyltartrate ((-)-DBT) was extracted more effectively than (+)-DBT.The enantioselectivity (α=D(-)
- Ohki, Akira,Miyashita, Ryo,Naka, Kensuke,Maeda, Shigeru
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p. 2714 - 2719
(2007/10/02)
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- α-Hydroxy thioethers
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Novel asymmetric thioethers of the formula STR1 in which the general symbols have the following meanings: a is an integer of from 1 to 7, Ro represents hydrogen or C1-7 -alkanoyl, R1 represents C1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C1-3 -perfluoroalkyl, R2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms, A represents ethylene or alternatively, if R1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene, B represents a single bond, ethynylene or phenylene, R3 represents hydroxy, C1-7 -alkoxy or an optionally substituted amino group, and --X-- represents a single bond, a methylene group of an optionally N-acylated primary aminomethylene group, and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
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- 4-oxo-benzopyran carboxylic acids
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Compounds of the Formula I: STR1 and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
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