| 摘要 |
organic chemistry, chemical technology. SUBSTANCE: invention proposes spiropiperidines of the formula (I) or (II) where R1 means aryl-(C1-C6-alkyl), C3-C7-cycloalkyl-(C1-C6-alkyl), aryl-(C0-C5-alkyl)-K-(C1-C6-alkyl), C3-C7-cycloalkyl-(C0-C5-alkyl)-K- -(C1-C5-alkyl) where K means O, S(O)m/ ; aryl means phenyl, pyridyl and indolyl that can be substituted with 1-2 halogen atoms; R2 is hydrogen atom; R3a and R3Ô are hydrogen, halogen atom, C1-C5-alkyl; R4 and R5 are hydrogen atom, C1-C6-alkyl substituted with 1-3 hydroxy-groups; R6 is hydrogen atom; A means the group -(CH2)x-C(R7)(R7a)- where x = 0 or 1; R7 and R7a mean C1-C6-alkyl being one of B, D, E, F means C(R8)(R10), O, C=O, S(O)m,NR9 being B, D, E or F can absent providing the formation of 5,6-membered ring; R8 and R10 mean hydrogen atom; R9 means -aryl where can be substituted with halogen atom, C1-C4-alkyl and others; is hydrogen atom or C1-C4-alkyl; q = 0, 1; m = 0, 1 or 2; n = 1; G, H, I and J mean carbon or sulfur atoms and at least one of that is heteroatom and one of G, H, I and J can absent optionally that provides the formation of 5-membered heterocyclic or 6-membered aromatic ring, and its pharmaceutical salts and individual diastereoisomers. Method of synthesis of compound of the formula (I) or (II) involves interaction of compound (4) or (4a) with compound of the formula HOOC-A-N-R4R5 or HOOC-A-N-(R4)L where L means protective group which is removed if it presents. Method of synthesis of compound of the formula (I) or (II) involves interaction of compound of the formula (2) or (2a) with compound of the formula (12) or (12a) where L means protective group which is removed. Synthesized compounds increase the content of endogenous growth hormone in humans and animals. Invention relates to also pharmaceutical composition used for increase of endogenous producing and secretion of human or animal growth hormone. EFFECT: improved methods of synthesis, valuable medicinal and pharmacological properties. 11 cl, 1 tbl, 56 ex
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