CPC C07K 1/1077 (2013.01) [A61K 38/07 (2013.01); A61K 47/64 (2017.08); A61K 47/6803 (2017.08); A61K 47/6849 (2017.08); A61K 47/6855 (2017.08); A61K 47/6889 (2017.08); C07F 9/448 (2013.01); C07F 9/4461 (2013.01); C07F 9/4473 (2013.01)] | 26 Claims |
1. A compound of formula (V)
wherein:
represents a triple bond;
X represents R3—C;
R1 independently represents an optionally substituted aliphatic or aromatic residue; optionally, R1 represents C1-C8-alkyl optionally substituted with at least one of (C1-C8-alkoxy)n wherein n is 1, 2, 3, 4, 5 or 6, F, Cl, Br, I, —NO2, —N(C1-C8-alkyl)H, —NH2, —N(C1-C8-alkyl)2, ═O, C3-C8-cycloalkyl, —S—S—(C1-C8-alkyl), hydroxy-(C1-C8-alkoxy)n wherein n is 1, 2, 3, 4, 5 or 6, C2-C8-alkynyl or optionally substituted phenyl; or
optionally, R1 represents phenyl optionally independently substituted with at least one of C1-C8-alkyl, (C1-C8-alkoxy)n wherein n is 1, 2, 3, 4, 5 or 6, F, Cl, I, Br, —NO2, —N(C1-C8-alkyl)H, —NH2 or —N(C1-C8-alkyl)2; or
optionally, R1 represents a 5- or 6-membered heteroaromatic system;
R3 represents H or C1-C8-alkyl;
and
● represents an aliphatic or aromatic residue.
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12. A process for the preparation of a compound of formula (V), said process comprising the steps of:
(I) reacting compound of formula (III)
wherein:
represents a double bond or a triple bond;
X represents R3—C when is a triple bond; or
X represents CR3(R4) when is a double bond;
R1 independently represents an optionally substituted aliphatic or aromatic residue;
optionally, R1 represents C1-C8-alkyl optionally substituted with at least one of (C1-C8-alkoxy)n wherein n is 1, 2, 3, 4, 5 or 6, F, Cl, Br, I, —NO2, —N(C1-C8-alkyl)H, —NH2, —N(C1-C8-alkyl)2, ═O, C3-C8-cycloalkyl, —S—S—(C1-C8-alkyl), hydroxy-(C1-C8-alkoxy)n wherein n is 1, 2, 3, 4, 5 or 6, C2-C8-alkynyl or optionally substituted phenyl; or
optionally, R1 represents phenyl optionally independently substituted with at least one of C1-C8-alkyl, (C1-C8-alkoxy)n wherein n is 1, 2, 3, 4, 5 or 6, F, Cl, I, Br, —NO2, —N(C1-C8-alkyl)H, —NH2 or —N(C1-C8-alkyl)2; or
optionally, R1 represents a 5- or 6-membered heteroaromatic system;
R3 represents H or C1-C8-alkyl; and
R4 represents H or C1-C8-alkyl;
with an azide of formula (IV)
wherein
● represents an aliphatic or aromatic residue;
to prepare a compound of formula (V)
wherein ●, , R1, and X are as defined above.
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