11-12-2014 дата публикации
Номер: US20140364339A1
Принадлежит:
The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). 4. The process according to claim 1 , wherein R2 is a hydrogen atom claim 1 , R3 is a Boc group claim 1 , R4 is phenyl and R5 is allyl.5. The process according to claim 1 , wherein the weak base is KPO claim 1 ,CsCOor KCO.6. The process according to claim 1 , wherein the solvent suitable for phase transition conditions is selected from the group consisting of chlorobenzene claim 1 , dichloromethane claim 1 , chloroform claim 1 , dichlorobenzene claim 1 , dichloroethane claim 1 , and dioxane.7. The process according to claim 1 , wherein R1 is selected from the group consisting of hydrogen atom claim 1 , allyl group and benzyl group.8. The process according to claim 1 , wherein R2 is a hydrogen atom or Boc and R3 is Boc.9. The process according to claim 1 , wherein the phosphine P(R4)is selected from the group consisting of tricyclohexylphosphine claim 1 , triphenylphosphine claim 1 , trifurylphosphine claim 1 , tri(4-methoxyphenyl)phosphine claim 1 , tri(4-trifluoromethylphenyl)phosphine claim 1 , tri(4-fluorophenylphosphine) and tri(4-chlorophenyl)phosphine.10. The process according to claim 1 , wherein RaCORb is selected from the group consisting of benzaldehyde claim 1 , 4-trifluoromethylbenzaldehyde claim 1 , 4-nitrobenzaldehyde claim 1 , 4-cyanobenzaldehyde claim 1 , 4-methoxybenzaldehyde claim 1 , 3 claim 1 ,4-dimethoxybenzaldehyde claim 1 , 2-furaldehyde claim 1 , 3-phenylpropanal claim 1 , paraformaldehyde claim 1 , phenylacetaldehyde claim 1 , 4-(4 claim 1 ,4 claim 1 ,5 claim 1 ,5-tetramethyl-1 claim 1 ,3 claim 1 ,2-dioxaborolan-2-yl)benzaldehyde claim 1 , aldehyde derived from calix-[4]-arene claim 1 , ferrocene-carboxaldehyde claim 1 , m- ...
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