cas 405-09-4, 2-Fluoro-4-methoxybenzyl alcohol

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Unusual Kinetic Profiles for Lewis Base-Catalyzed Sulfenocyclization of ortho -Geranylphenols in Hexafluoroisopropyl Alcohol
The kinetic behavior of the Lewis base-catalyzed sulfenocyclization of polyenes in hexafluoroisopropyl alcohol (HFIP) was explored. The rate of reaction is not dependent on the electronic properties of the terminal nucleophile, suggesting that this captur
Robb, Kevin A.,Athavale, Soumitra V.,Denmark, Scott E.
supporting information
p. 1656 - 1661
(2019/08/26)

Isoindoline derivative and intermediate, preparation method, pharmaceutical composition and application thereof
The invention discloses an isoindoline derivative, and an intermediate, a preparation method, a pharmaceutical composition and application thereof. The isoindoline derivative of the invention and the pharmaceutical composition thereof can adjust productio
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Paragraph 0289; 0290

(2016/10/08)

PHARMACEUTICAL COMPOSITION COMPRISING A PYRAZOLE-O-GLUCOSIDE DERIVATIVE
The invention relates toa pharmaceutical composition comprising a pyrazole-O-glucoside derivative selected from the group of compounds (1) to (29) according to claim 1 in combination with at least one second therapeutic agent which is suitable in the trea
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Page/Page column 47-48

(2008/12/07)

METHODS FOR PREVENTING AND TREATING METABOLIC DISORDERS AND NEW PYRAZOLE-O-GLYCOSIDE DERIVATIVES
The invention relates to methods for preventing or treating metabolic disorders, for improving glycemic control, for preventing progression from impaired glucose tolerance, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, for
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Page/Page column 33; 34

(2010/11/25)

Synthesis, biological evaluation and molecular modeling studies of N6-benzyladenosine analogues as potential anti-toxoplasma agents
Toxoplasma gondii is an opportunistic pathogen responsible for toxoplasmosis. T. gondii is a purine auxotroph incapable of de novo purine biosynthesis and depends on salvage pathways for its purine requirements. Adenosine kinase (EC.2.7.1.20) is the major enzyme in the salvage of purines in these parasites. 6-Benzylthioinosine and analogues were established as "subversive substrates" for the T. gondii, but not for the human adenosine kinase. Therefore, these compounds act as selective anti-toxoplasma agents. In the present study, a series of N6-benzyladenosine analogues were synthesized from 6-chloropurine riboside with substituted benzylamines via solution phase parallel synthesis. These N6-benzyladenosine analogues were evaluated for their binding affinity to purified T. gondii adenosine kinase. Furthermore, the anti-toxoplasma efficacy and host toxicity of these compounds were tested in cell culture. Certain substituents on the aromatic ring improved binding affinity to T. gondii adenosine kinase when compared to the unsubstituted N6-benzyladenosine. Similarly, varying the type and position of the substituents on the aromatic ring led to different degrees of potency and selectivity as anti-toxoplasma agents. Among the synthesized analogues, N6-(2,4-dimethoxybenzyl)adenosine exhibited the most favorable anti-toxoplasma activity without host toxicity. The binding mode of the synthesized N6-benzyladenosine analogues were characterized to illustrate the role of additional hydrophobic effect and van der Waals interaction within an active site of T. gondii adenosine kinase by induced fit molecular modeling.
Kim, Young Ah,Sharon, Ashoke,Chu, Chung K.,Rais, Reem H.,Al Safarjalani, Omar N.,Naguib, Fardos N.M.,el Kouni, Mahmoud H.
p. 1558 - 1572
(2008/02/08)

PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
A compound of the formula wherein R1 is a heterocycle having a skeleton consisting of 3 to 15 atoms including 1 to 5 nitrogen atom(s), which heterocycle is attached by a secondary nitrogen atom constituting the heterocycle; X is an oxygen atom, a nitrogen atom optionally substituted by a hydrocarbon group having 1 to 5 carbon atom(s) or a sulfur atom optionally oxidized with 1 or 2 oxygen, Y is a bond or a C1-5 alkylene group, R2 is (1) a hydrogen atom, (2) a hydroxy group, (3) a C1-5 alkoxy group, (4) a C1-5 alkylthio group, (5) a carbocycle having 3 to 15 carbon atoms or (6) a heterocycle having a skeleton consisting of 3 to 15 atoms including 1 to 5 heteroatom(s), provided that when Y is a bond, R2 is a carbocycle having 3 to 15 carbon atoms or a heterocycle having a skeleton consisting of 3 to 15 atoms including 1 to 5 heteroatom(s) and; one of R3 and R4 is a hydrogen atom or a group of the formula: -Z-R5 (Z is a bond or C1-10 alkylene group optionally having substituent(s) and R5 is (1) a hydrogen atom, (2) a hydroxy group, (3) a C1-5 alkoxy group, (4) a nitrile group, (5) a C1-5 alkoxy-carbonyl group, (6) a carboxyl group, (7) a carbamoyl group, (8) a (mono or di-C1-5 alkyl)carbamoyl group, (9) an amino group, (10) a (di or mono-C1-5 alkyl)amino group, (11) a (C1-5 alkoxy-carbonyl)amino group, (12) a C1-5 alkylthio group, (13) a carbocycle having 3 to 15 carbon atoms or (14) a heterocycle having a skeleton consisting of 3 to 15 atoms including 1 to 5 heteroatom(s)); the other is a group of the formula: -Z-R5 (Z and R5 are as defined above); and R3 and R4 may form, together with the adjacent nitrogen atom, a heterocycle having a skeleton consisting of 3 to 15 atoms, which heterocycle is attached by a secondary nitrogen atom constituting the heterocycle, wherein the above-mentioned heterocycle and a carbocycle having 3 to 15 carbon atoms are each optionally substituted by substituent(s) selected from the group consisting of C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C7-16 aralkyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C6-14 aryl, C1-8 alkoxy, C1-3 alkylenedioxy, hydroxy, halogen atom, amino, (di or mono-C1-5 alkyl)amino, (C1-5 alkoxy-carbonyl)amino, (C1-5 acyl)amino, (C1-5 acyl) (C1-5 alkyl)amino, C1-5 alkylthio, nitrile, nitro, C1-5 alkoxy-carbonyl, carboxyl, C1-5 alkyl-carbonyloxy, oxo, thioxo, C1-6 acyl group, sulfamoyl and (di or mono-C1-5 alkyl)sulfamoyl, or a salt thereof or a prodrug thereof have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the prophylaxis or treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis and the like, allergic diseases such as asthma, or disorders of male or female genital function and the like.
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(2008/06/13)

Nitrone derivatives
A compound represented by the figure (1) or a pharmaceutically acceptable salt thereof is useful as medicament for treating retinal degenerative disorders: wherein Ar is optionally substitued phenyl or optionally substituted heteroaryl;. n is 0, 1 or 2; W
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(2008/06/13)

Asymmetric synthesis of fluorinated L-tyrosine and meta-L-tyrosines
A convenient asymmetric synthesis of (2S)-2-amino-3-(2-fluoro-5-hydroxyphenyl) propanoic acid, (2S)-2-amino-3-(4-fluoro-3-hydroxyphenyl) propanoic acid and (2S)-2-amino-3-(2-fluoro-4-hydroxyphenyl) propanoic acid is described.Key steps include the synthes
Monclus, Michel,Masson, Carine,Luxen, Andre
p. 39 - 44
(2007/10/02)

Aqua(sulfato)platinum(II) Complexes with Variable Substituents in the 2-Phenyl Ring. 1. Synthesis and Antitumor and Estrogenic Properties
Erythro- and threo-configurated aqua(sulfato)platinum(II) complexes with variable substituents in the 2-phenyl ring (2-PtSO4 to 9-PtSO4: H, 4-F, 3-OH, 4-OH, 2,6-F2, 2,6-Cl2, 2-F/4-OH, 2-Cl/4-OH) were synthesized and tested for estrogenic and antitumor activities.The ligands were obtained by a three-step reaction.The stilbenes were reacted with a mixture of IN3 and NaN3 to yield the respective 1,2-diazido-1,2-diphenylethanes.The subsequent reduction with LiAlH4 led to the corresponding 1,2-diphenylethylenediamines.The (sulfato)platinum(II) complexes were synthesized by reaction of Ag2SO4 with the diiodo complexes, which had been obtained by coordination of the diamines with K2PtI4.Two complexes, erythro-8-PtSO4 and erythro-9-PtSO4, possess antitumor and estrogenic effects and are therefore of interest for the therapy of breast cancer.
Gust, Ronald,Burgemeister, Thomas,Mannschreck, Albrecht,Schoenenberger, Helmut
p. 2535 - 2544
(2007/10/02)