- Calcipotriol intermediate compound and preparation method thereof
-
The invention discloses a calcipotriol intermediate compound and a preparation method thereof. The structure of the compound is represented by general formula I shown in the description. In the general formula I, R1 is selected from a carbobenzoxy group (Cbz), a trimethylsilyl group (TMS), a triethylsilyl group (TES), a t-butyldimethylsilyl group (TBDMS), a triisopropylsilyl group (TIPS), a t-butyl-diphenylsilyl group (TBDPS) or a methoxymethyl group (MOM); and R2 is one of groups shown in the description.
- -
-
-
- Enantioselective synthesis of iclaprim enantiomers- A versatile approach to 2-substituted chiral chromenes
-
Figure presented Both enantiomers of the DHFR inhibitor iclaprim (R)-1 and (S)-1 were synthesized from the cyclopropyl homoallyl alcohols (R)-6 and (S)-6, respectively. As key steps these transformations include a Mitsunobu reaction and the formation of the diaminopyrimidine unit prior to a novel cyclization procedure to obtain the desired chromene heterocycle. The moderate enantioselectivity of the products (R)-1 and (S)-1 is related to the Mitsunobu reaction, which unfortunately did not proceed with complete inversion of configuration.
- Tahtaoui, Chouaib,Demailly, Arnold,Guidemann, Carole,Joyeux, Cecile,Schneider, Peter
-
supporting information; experimental part
p. 3781 - 3785
(2010/09/03)
-
- PREPARATION OF 24 ALKYL ANALOGS OF CHOLECALCIFEROL AND NON-RACEMIC COMPOUNDS
-
Disclosed is a process for the preparation of 24 -alkyl analogs of cholecalcyferol of Formula 1 having a (5E) or (5Z) configuration, wherein X represents a hydrogen atom, a hydroxy group or an OR1 group, wherein R1, R2
- -
-
-