375368-91-5

Upstream product

• 2646-90-4 2,5-difluorobenzaldehyde 
• 1099-45-2 ethyl (triphenylphosphoranylidene)acetate 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 

Downstream Products

• 872263-26-8 (E)-3-(2,5-difluorophenyl)acrylaldehyde 
• 1093218-54-2 {(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthyridin-4-yl)-ethyl]-tetrahydropyran-3-yl}-[3-(2,5-difluorophenyl)-allyl]-amine 
• 1093218-81-5 {(3R,6S)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthyridin-4-yl)-ethyl]-tetrahydropyran-3-yl}-[(E)-3-(2,5-difluorophenyl)-allyl]-amine 
• 1093219-10-3 [(1RS)-1-{(2S,5R)-5-[(E)-3-(2,5-difluoro-phenyl)-allylamino]-tetrahydropyran-2-yl}-2-(6-methoxy[1,5]naphthyridin-4-yl)-ethyl]-carbamic acid benzyl ester 

Relevant academic research and scientific papers

Solventless Wittig olefination with fluorinated benzaldehydes

Fluorinated benzaldehydes undergo solventless Wittig olefination with stabilised phosphoranes. Even with less reactive, stabilised phosphoranes, such as acetylmethylidenetriphenylphosphorane, the reactions have been found to be exothermic.

Studies directed toward the exploitation of vicinal diols in the synthesis of (+)-nebivolol intermediates

While the exploitation of the Sharpless asymmetric dihydroxylation as the source of chirality in the synthesis of acyclic molecules and saturated heterocycles has been tremendous, its synthetic utility toward chiral benzo-annulated heterocycles is relatively limited. Thus, in the search for wider applications of Sharpless asymmetric dihydroxylation-derived diols for the synthesis of benzo-annulated heterocycles, we report herein our studies in the asymmetric synthesis of (R)-1-((R)-6-fluorochroman-2-yl)ethane-1,2-diol, (R)-1-((S)-6-fluorochroman-2-yl)ethane-1,2-diol and (S)-6-fluoro-2-((R)-oxiran-2-yl)chroman, which have been used as late-stage intermediates for the asymmetric synthesis of the antihypertensive drug (S,R,R,R)-nebivolol. Noteworthy is that a large number of racemic and asymmetric syntheses of nebivolol and their intermediates have been described in the literature, however, the Sharpless asymmetric dihydroxylation has never been employed as the sole source of chirality for this purpose.

4-(1-AMINO-ETHYL)-CYCLOHEXYLAMINE DERIVATIVES

The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 /su

4-(1-AMINO-ETHYL)-CYCLOHEXYLAMINE DERIVATIVES

The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2/sup

3-AMINO-6-(1-AMINO-ETHYL)-TETRAHYDROPYRAN DERIVATIVES

The invention relates to antibacterial compounds of formula I wherein R1 represents halogen or alkoxy; U and W each represent N, V represents CH and R2 represents H or F, or U and V each represent CH, W represents N and R2

New Piperidine Antibiotics

The invention relates to novel, antibacterially active piperidine derivatives of the formula wherein one of U and V represents N, the other represents N or CH; M represents CH2CH2, CH═CH, CH(OH)CH(OH), CH(OH)CH2, CH(NHsub

TETRAHYDROPYRANE ANTIBIOTICS

The invention relates to antibiotic tetrahydro rane derivatives of formula (I).

ANTIBIOTIC COMPOUNDS

The invention relates to selected antibiotics of formula (Al) wherein R1 represents alkyl, alkoxy, haloalkoxy, halogen or cyano; one or two of U, V, W and X represent(s) N, the remaining represent CH, or, in case of U, V and/or W, may also repr

ETHANOL OR 1,2-ETHANEDIOL CYCLOHEXYL ANTIBIOTIC DERIVATIVES

The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represent(s) N and the remaining represent each independently CH or, in the case of V or X

NEW PIPERIDINE ANTIBIOTICS

The invention relates to novel, antibacterially active piperidine derivatives of the formula (I) wherein one of U and V represents N, the other represents N or CH; M represents CH2CH2, CH=CH, CH(OH)CH(OH), CH(OH)CH2, CH(NH