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First Claim
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1. Vitamin D derivatives of general formula I, in which Y1 means a hydrogen atom, a hydroxyl group, a fluorine, chlorine or bromine atom or a group —
- OCOR8, in which R8 is an aliphatic or aromatic radical with 1 to 12 C atoms, Y2 means a hydrogen atom or a group —
(CO)R9, in which R9 is an aliphatic or aromatic radical with 1 to 12 C atoms, R1 and R2 each mean a hydrogen atom or together an exocyclic methylene group, R3 and R4, independently of one another, mean a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1 to 4 carbon atoms, together a methylene group or together with quaternary carbon atom 20 a 3- to 7-membered, saturated or unsaturated carbocyclic ring, V and W together mean an E-double bond or V means a hydroxyl group and W means a hydrogen atom, Q means a straight-chain or branched carbon unit with up to 10 carbon atoms, which at any positions can have α
- or β
-hydroxyl groups, which in turn can be etherified or esterified, keto groups, amino groups or halogen atoms, Z means a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 12 carbon atoms, which at any positions can have keto groups, α
- or β
-hydroxyl groups, which in turn can be etherified or esterified, amino groups, fluorine, chlorine, or bromine atoms.
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Abstract
The invention relates to new vitamin D derivatives of general formula (I), process for their production, intermediate products of the process as well as the use for production of pharmaceutical agents.
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Citations
13 Claims
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1. Vitamin D derivatives of general formula I,
in which Y1 means a hydrogen atom, a hydroxyl group, a fluorine, chlorine or bromine atom or a group — - OCOR8, in which
R8 is an aliphatic or aromatic radical with 1 to 12 C atoms, Y2 means a hydrogen atom or a group —
(CO)R9, in whichR9 is an aliphatic or aromatic radical with 1 to 12 C atoms, R1 and R2 each mean a hydrogen atom or together an exocyclic methylene group, R3 and R4, independently of one another, mean a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1 to 4 carbon atoms, together a methylene group or together with quaternary carbon atom 20 a 3- to 7-membered, saturated or unsaturated carbocyclic ring, V and W together mean an E-double bond or V means a hydroxyl group and W means a hydrogen atom, Q means a straight-chain or branched carbon unit with up to 10 carbon atoms, which at any positions can have α
- or β
-hydroxyl groups, which in turn can be etherified or esterified, keto groups, amino groups or halogen atoms,Z means a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 12 carbon atoms, which at any positions can have keto groups, α
- or β
-hydroxyl groups, which in turn can be etherified or esterified, amino groups, fluorine, chlorine, or bromine atoms. - View Dependent Claims (2, 3, 4, 5, 12)
- OCOR8, in which
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6. Process for the production of vitamin D derivatives of general formula I, whereby a compound of general formula II
in which Y′ -
1 means a hydrogen atom, a halogen atom, or a protected hydroxyl group and Y′
2 means a hydroxy protective group, is converted into the compound of general formula I by simultaneous or successive cleavage of the hydroxy and keto protective groups and optionally by partial or complete esterification of free hydroxyl groups.
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1 means a hydrogen atom, a halogen atom, or a protected hydroxyl group and Y′
- 7. Use or the vitamin D derivatives of general formula I for the production of pharmaceutical agents.
Specification