84983-97-1Relevant articles and documents
COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 19, (2010/11/30)
The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt or solvate thereof: wherein n, m and p, which may be the same or different, are either 0 or 1. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and their use as medicaments particularly in treating disorders of the central nervous system (CNS).
COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 31-32, (2010/11/30)
The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R2 is C1-6alkyl, C3-6cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R3 is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxyC1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-6alkyl; R5 is hydrogen; or R5 and R3, together with the nterconnecting atoms, form a 4, 5 or 6 membered ring; R6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and heir use as medicaments particularly in treating disorders of the Central Nervous System (CNS).
Synthesis of (S)- and (R)-1-(2-furyl)alkylamines and (S)- and (R)-α- amino acids through the addition of organometallic reagents to imines derived from (S)-Valinol
Alvaro, Giuseppe,Martelli, Gianluca,Savoia, Diego,Zoffoli, Andrea
, p. 1773 - 1777 (2007/10/03)
(S)-1-(2-Furyl)alkylamines were prepared through the addition of organometallic reagents to the imine derived from 2-furaldehyde and (S)- valinol, previous protection of the auxiliary hydroxy group as trimethylsilyl ether, followed by removal of the auxiliary. Then, protection of the primary amine as tosylamide or benzamide and oxidation of the furan ring gave the N- derivatives of (S)-α-amino acids. (R)-N-Benzoylphenylglycine was prepared from the benzaldimine, where the hydroxy group was protected as the tert- butyldimethylsilyl ether, through addition of 2-furyllithium.