351418-50-3

Upstream product

• 288-32-4 1H-imidazole 
• 2973-80-0 2-bromo-5-hydroxybenzaldehyde 
• 12125-02-9 ammonium chloride 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 100-83-4 meta-hydroxybenzaldehyde 

Downstream Products

• 906673-48-1 2-bromo-5-tert-butyldimethylsiloxybenzylalcohol 
• 906673-51-6 1-bromo-4-tert-butyldimethylsiloxy-2-methoxymethoxymethylbenzene 
• 1187190-70-0 1,3-dihydro-1,5-dihydroxy-2,1-benzoxaborolane 
• 906673-24-3 AN₂₇₂₈ 
• 1393367-77-5 (Z)-(4-bromo-3-(2-bromovinyl)phenoxy)(tert-butyl)dimethylsilane 
• 1393367-76-4 (E)-(4-bromo-3-(2-bromovinyl)phenoxy)(tert-butyl)dimethylsilane 

Relevant academic research and scientific papers

Preparation method of crisaborole

The invention discloses a preparation method of crisaborole, which comprises the following steps: S1, reacting 2-bromo-5-hydroxybenzaldehyde with a hydroxyl protecting reagent in a solvent in the presence of alkali to obtain a compound I; S2, reducing the compound I in a solvent in the presence of a reducing agent to obtain a compound I I; S3, reacting the compound I with a hydroxyl protection reagent in a solvent in the presence of alkali to obtain a compound IV; S4, reacting the compound IV with boric acid ester in a solvent in the presence of alkali to obtain a compound V; S5, removing a hydroxyl protecting group from the compound V to obtain a compound VI; and S6, reacting the compound IV with p-fluorobenzonitrile to obtain crisaborole. A hydroxyl protecting group which is more beneficial to removal is adopted in the route, synthesis of boric acid ester is facilitated, side reactions are reduced, the yield is obviously increased, and the method is easy to operate, low in cost and beneficial to industrial production.

Synthesis of Monodisperse Naphthalene Dendrons for the Application of Dendrimers

Syntheses of dendrons for dendrimer applications are described using napthyl and urethane derivatives. The napthol, 1-(3-hydroxy-6-(methoxymethoxy)naphthalen-1-yl)ethan-1-one (h), was synthesized by employing Au-catalyzed cyclization of the corresponding

Synthesis of Complex Stereoheptads en Route to Daphnane Diterpene Orthoesters

Tricyclic cores of the daphnane diterpene orthoesters (DDOs) are synthesized in 10 steps from readily available materials. Key to their assembly is the development of a stereocontrolled p-quinol functionalization sequence which enables rapid access to DDO C-ring stereopolyads from simple precursors. Problems encountered in stereo- and regioselectivity are highlighted and solved by exact changes in choreography, although it is shown that the undesired stereochemical outcomes also proceed with high selectivity.

Boron-Containing Small Molecules as Anti-Inflammatory Agents

Compounds and methods of treating anti-inflammatory conditions are disclosed.

1H-phosphindoles as structural units in the synthesis of chiral helicenes

Building helicenes: A photochemical cyclization approach affords helicenes in which the fused ring sequence ends with a phosphole unit (see scheme). The stereogenic phosphorus centers of the substrates control the screw sense of helical chirality. The terminal phosphole units undergo photochemical [2+2] annulations to give dimeric helical structures. Copyright

Survivin inhibitors

Compounds that inhibit survivin, compositions containing the compounds and methods of treating diseases in which survivin is unregulated or overexpressed are disclosed.

Use of molecular weight-enlarged catalysts in a process for asymmetric, continous hydrogenation, novel molecular weight-enlarged ligands and catalysts

The first embodiment of the present invention provides a process, which includes: in a continuous process in a membrane reactor, asymmetrically hydrogenating at least one C=C, C=N or C=O double bond with a catalyst. Another embodiment of the present invention provides a ligand, which includes at least one di-1,3-aminophosphine homochiral active center; optionally, a linker; and a molecular weight-enlarging polymer; wherein the active center is bound to the molecular weight-enlarging polymer through the linker or is bound directly to the molecular weight-enlarging polymer; and wherein the linker is defined in the claims. Another embodiment of the present invention provides a process for preparing the above-noted ligand, and a catalyst that includes the above-noted ligand.

Continuous Application of Chemzymes in a Membrane Reactor: Asymmetric Transfer Hydrogenation of Acetophenone

The application of homogeneously soluble catalysts is limited by the recovery in cases where the price of the catalyst is high. Biological catalysts, enzymes, can be efficiently recycled by means of an ultrafiltration membrane due to their high molecular weight, for example, in the continuously operated membrane reactor. In order to transfer this principle to chemical catalysis, we have attached a transfer hydrogenation catalyst, first invented by Gao and Noyori, to a polymer. The resulting homogeneously soluble, polymer-bound catalyst (chemzyme) can now be retained by ultrafiltration membranes like enzymes. On applying this catalyst in continuously operated membrane reactors, a continuous isopropoxide dosage is necessary in order to compensate deactivation caused by water residues in the feed stream. Thus, high space-time yields up to 578 g L-1 d-1 and enantioselectivities up to 94% can he achieved. These results were compared to an enzyme catalyzed system consisting of a carbonyl reductase that also utilizes 2-propanol as a hydrogen source for the cofactor regeneration of NADH.