- Native Amine-Directed ortho -C-H Halogenation and Acetoxylation /Condensation of Benzylamines
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Free or unfunctionalized benzylamines are well known to participate in C-H activation in the presence of palladium salts. Despite the ease with which these complexes can be activated, subsequent functionalization of the dimeric cyclometalates can be chall
- Chand-Thakuri, Pratibha,Alahakoon, Indunil,Liu, Daniel,Kapoor, Mohit,Kennedy, John F.,Jenkins, Kenneth W.,Rabon, Allison M.,Young, Michael C.
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p. 341 - 354
(2021/10/07)
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- 5-ARYL-1-IMINO-1-OXO-[1,2,4]THIADIAZINES
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The present invention provides a compound of formula I' having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are
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Page/Page column 44; 45
(2015/07/07)
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- 5-AMINO[1,4]THIAZINES AS BACE 1 INHIBITORS
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The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
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Page/Page column 35
(2014/01/07)
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- Water soluble phosphines: Part XIII. Chiral phosphine ligands with amino acid moieties
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Nucleophilic phosphination of the potassium or sodium salt of the fluorophenylalanines (1a, 2a) or -glycines (3a, 4a) with potassium phosphides Ph(R)PK (R=Me, Ph) yields chiral phosphine ligands (1-7) with amino acid moieties. The X-ray structure of 3·2H2O (space group Pbca) has been determined showing a betaine type structure for the amino acid moiety. The α-methyl derivatives of the phosphinophenylglycines (10, 11) were obtained in an analogous manner as 1-7. ortho- and para-Fluoroacetophenones have been employed as starting material for the syntheses of α-[4-fluorophenyl]-α-methylglycine (9c) and its ortho-isomer (8c), the X-ray structure of its monohydrate has been determined (space group P1?). The N-acetyl (3b, 8e) and ester derivatives (3d, 8d) of 3 and 8c are accessible using standard procedures. Resolution of the diastereomeric salt 12 obtained from (S)-(+)-2-hydroxymethylpyrrolidine and racem-8e by fractionated crystallization yielded the (S,R)-isomer. The absolute configuration of (S,R)-12 was determined by X-ray structural analysis (space group P212121). Cleavage of (S,R)-12 with hydrochloric acid gave enantiopure (R)-8e [α]D20=-30.9° (c=1, CH3OH).
- Brauer, David J.,Schenk, Stefan,Ro?enbach, Stefan,Tepper, Michael,Stelzer, Othmar,H?usler, Thomas,Sheldrick, William S.
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p. 116 - 126
(2007/10/03)
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