606129-69-5Relevant articles and documents
Asymmetric synthesis of (s)-3-amino-4-methoxy-butan-1-ol by way of reductive amination
Mattei, Patrizio,Moine, Gerard,Puentener, Kurt,Schmid, Rudolf
, p. 353 - 359 (2012/05/19)
A new synthesis of (S)-3-amino-4-methoxy-butan-1-ol is reported. The synthesis is based on the preparation of the primary, nonprotected enamine of the commercially available β-keto ester methyl 4-methoxy-3-oxo-butanoate and asymmetric catalytic enamine hydrogenation using a Ru-MeOBIPHEP catalyst. Alternatively, the process is performed by asymmetric catalytic reductive amination of the β-keto ester with ammonium acetate and hydrogen using a similar Ru catalyst. Both process versions provided initial ee values of 97-98% which were upgraded to ≥99% by product crystallization. Ester to alcohol conversion was best accomplished by LiBH4 reduction after transitory Boc protection of the amino group.
1,3-DISUBSTITUTED AZETIDINE DERIVATIVES FOR USE AS CCR-3 RECEPTOR ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISEASES
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Page 32, (2010/02/11)
Compounds of formula Ia or Ib in free or salt form, wherein Ar, X1, X2, m, R1, Q, Y, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by CCR-3, for example an inflammatory or allergic cond