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Synthesis and preliminary biological evaluation of 20-epi-eldecalcitol [20-epi-1α,25-dihydroxy-2β-(3-hydroxypropoxy)vitamin D3: 20-epi-ED-71]
In the induction of human myeloid leukemia cell differentiation, inhibition of the human histiocytic lymphoma cell proliferation, and increase in osteocalcin concentration in the human osteosarcoma cell (MG-63), 20-epi-eldecalcitol showed significantly enhanced activity compared to eldecalCitol. Expand
β-Isocupreidine–hexafluoroisopropyl acrylate method for asymmetric Baylis–Hillman reactions
Abstract Key features of the β-isocupreidine (β-ICD)-catalyzed asymmetric Baylis–Hillman reaction of aldehydes with 1,1,1,3,3,3-hexafluoroisopropyl acrylate (HFIPA) are presented. In addition, anExpand
Synthesis and biological evaluation of a 3-positon epimer of 1alpha,25-dihydroxy-2beta-(3-hydroxypropoxy)vitamin D3 (ED-71).
Synthesis of 3-epi-ED-71 and investigations of in vitro suppression of PTH using bovine parathyroid cells are described and ED-71 showed weak activity towards PTH suppression in the authors' assays. Expand
Synthesis and biological evaluation of a 3-positon epimer of 1α,25-dihydroxy-2β-(3-hydroxypropoxy)vitamin D3 (ED-71)
1alpha,25-Dihydroxy-2beta-(3-hydroxypropoxy)vitamin D(3) (ED-71), an analog of active vitamin D(3), 1alpha,25-dihydroxyvitamin D(3) [1,25(OH)(2)D(3)], possesses a hydroxypropoxy substituent at theExpand
Total synthesis of neooxazolomycin.
β-Isocupreidine-Catalyzed Baylis−Hillman Reaction of Chiral N-Boc-α-Amino Aldehydes
β-Isocupreidine (β-ICD)-catalyzed Baylis−Hillman reaction of chiral N-Boc-α-amino aldehydes and 1,1,1,3,3,3-hexafluoroisopropyl acrylate (HFIPA) takes place without racemization and exhibits the ma...
Total synthesis of oxazolomycin A.
The first total synthesis of oxazolomycin A, a structurally novel oxazole polyene γ-lactam/β-lactone antibiotic, is described. Key features include the stereocontrolled construction of the right-handExpand
Two Convergent Approaches to the Synthesis of 1α,25-Dihydroxy-2β-(3-hydroxypropoxy)vitamin D3 (ED-71) by the Lythgoe and the Trost Coupling Reactions
Two convergent syntheses of 1α,25-dihydroxy-2β-(3-hydroxypropoxy)vitamin D 3 (ED-71) by the Lythgoe coupling reaction between the A-ring phosphine oxide and the C/D-ring ketone and the Trost couplingExpand
Asymmetric total synthesis of (+)-phoslactomycin B.
The synthetic method developed enables us to synthesize three other isomers concerning the C11-OH and Delta12-double bond. Expand