81036-83-1

Upstream product

• 53392-07-7 4-(4-methylphenyl)butan-1-ol 
• 4619-20-9 3-(4-methylbenzoyl)propionic acid 
• 108-88-3 toluene 
• 627-27-0 homoalylic alcohol 
• 624-31-7 4-tolyl iodide 
• 3333-13-9 p-allyltoluene 
• 201230-82-2 carbon monoxide 
• 24306-23-8 methyl 4-(4-methylphenyl)butanoate 
• 31208-53-4 4-p-tolylbut-3-yn-1-ol 
• 4521-22-6 4-(4-methylphenyl)butyric acid 
• 122-51-0 orthoformic acid triethyl ester 
• 81036-82-0 4-(4-bromophenyl)butyraldehyde 
• 74-88-4 methyl iodide 

Downstream Products

• 183129-91-1 [2-Amino-5-(2-p-tolyl-ethyl)-thiophen-3-yl]-(2-chloro-phenyl)-methanone 
• 183130-07-6 2-Amino-N-[3-(2-chloro-benzoyl)-5-(2-p-tolyl-ethyl)-thiophen-2-yl]-acetamide 
• 183129-99-9 2-Chloro-N-[3-(2-chloro-benzoyl)-5-(2-p-tolyl-ethyl)-thiophen-2-yl]-acetamide 
• 1027270-89-8 N-[3-(2-Chloro-benzoyl)-5-(2-p-tolyl-ethyl)-thiophen-2-yl]-2-iodo-acetamide 
• 117280-11-2 5-(2-Chloro-phenyl)-7-(2-p-tolyl-ethyl)-1,3-dihydro-thieno[2,3-e][1,4]diazepin-2-one 
• 117280-12-3 5-(2-Chloro-phenyl)-7-(2-p-tolyl-ethyl)-1,3-dihydro-thieno[2,3-e][1,4]diazepine-2-thione 
• 117280-13-4 [5-(2-Chloro-phenyl)-7-(2-p-tolyl-ethyl)-1,3-dihydro-thieno[2,3-e][1,4]diazepin-(2Z)-ylidene]-hydrazine 
• 1200112-66-8 ethyl (2E)-2-methyl-6-(4-methylphenyl)-2-hexenoate 
• 1332954-73-0 (E)-6-(p-tolyl)hex-3-en-1-ol 

Relevant academic research and scientific papers

Direct Access to N-tert-Butanesulfinyl Imines from Aryl Iodides, Alkenyl Alcohols, and N-tert-Butanesulfinamide

The reaction of aryl iodides, N-tert-butanesulfinamide, and allyl or homoallyl alcohol in the presence of a catalytic amount of Pd(OAc)2, NaHCO3 as a base, and TBAB leads to the formation of N-tert-butanesulfinyl imines in moderate yields. In this one-pot process, a sequential Heck-type arylation of the alkenol, isomerization of the double bond, and imine formation take place.

Ligand-controlled cobalt-catalyzed remote hydroboration and alkene isomerization of allylic siloxanes

The Co-catalyzed remote hydroboration and alkene isomerization of allylic siloxanes were realized by a ligand-controlled strategy. The remote hydroboration with dcype provided borylethers, while xantphos favored the formation of silyl enol ethers.

Copper(I)-catalyzed stereodivergent propargylation of N-acetyl mannosamine for protecting group minimal synthesis of C3-substituted sialic acids

Copper(I)-catalyzed stereodivergent nucleophilic propargylation at the anomeric carbon of unprotected N-acetyl mannosamine was developed using 3-substituted allenylboronates as a nucleophile. The homopropargylic alcohol products contained two contiguous s

Chiral geminal disilyl alkane compound, synthesis method and applications thereof

The present invention discloses a chiral geminal disilyl alkane compound, which is represented by a formula V, wherein * represents a chiral carbon atom in the formula V. The invention discloses a synthesis method of the chiral geminal disilyl alkane compound, wherein the synthesis method comprises: carrying out a reaction in the presence of a reducing agent by using alkyne represented by a formula I, dihydrosilane represented by a formula II and trihydrosilane represented by a formula III as raw materials and using Xantphos-CoBr2 and a chiral CoX2-OIP complex as catalysts under an inert gas to prepare the chiral geminal disilyl alkane compound represented by the formula V. According to the present invention, the method has characteristics of mild reaction condition, simple operation, highatomic economy, no requirement of the addition of any other toxic transition metals (such as ruthenium, rhodium, palladium and the like) salts, high yield and high enantioselectivity, and has great practical value in the synthesis of drugs and materials, wherein the yield is generally 50-85%, and the enantioselectivity is generally 93-99%. The formulas I, II, III and V are defined in the specification.

Racemic gem disilyl alkane compound containing four silicon-hydrogen bonds, and sybthesis method and application of compound

The invention discloses a racemic gem disilyl alkane compound containing four silicon-hydrogen bonds. The compound is as shown in a formula IV. The invention further discloses a synthesis method of the racemic gem disilyl alkane compound. The synthesis method comprises the following step of carrying out a reaction by taking alkyne as shown in a formula I and trihydrosilane as shown in a formula IIas raw materials and taking a chiral CoX-IIP complex as a catalyst in the presence of a reducing agent to obtain the racemic gem disilyl alkane compound containing four silicon-hydrogen bonds, wherein the compound is as shown in the formula IV. The method disclosed by the invention has mild reaction conditions, is simple and convenient to operate and has high atom economy. In addition, the reaction does not need addition of any salts of toxic transition metals (such as ruthenium, rhodium, palladium and the like), and the method has a relatively large practical application value in synthesis of medicines and materials. In addition, the reaction has a medium to excellent yield (51-99%) and high area selectivity (10:1-19:1, most parts larger than 19:1).

Rhodium/Phosphine catalysed selective hydroformylation of biorenewable olefins

This work reports rhodium catalyzed selective hydroformylation of natural olefins like eugenol, estragole, anethole, prenol and isoprenol using biphenyl based Buchwald phosphine ligands (S-Phos (L1), t-Bu XPhos (L2), Ru-Phos (L3), Johnphos (L4) and DavePhos (L5). Ru-Phos (L3) ligand exhibited high impact on the hydroformylation of eugenol providing high selectivity (90%) of linear aldehyde as major product. In addition, internal natural olefins like anethole and prenol provided moderate to high selectivity (65% and 85% respectively) of branched aldehydes as a major products. The various reaction parameters such as influence of ligands, P/Rh ratio, syngas pressure, temperature, time and solvents have been studied. A high activity and selectivity gained on the way to the linear aldehydes it may be due to the bulky, steric cyclohexyl and isopropoxy groups present in L3 phosphine ligand. Moreover, this catalytic system was smoothly converting natural olefins into corresponding linear and branched aldehydes with higher selectivity under the mild reaction conditions.

Targeting an Aromatic Hotspot in Plasmodium falciparum 1-Deoxy-d-xylulose-5-phosphate Reductoisomerase with β-Arylpropyl Analogues of Fosmidomycin

Blocking the 2-C-methyl-d-erythrithol-4-phosphate pathway for isoprenoid biosynthesis offers new ways to inhibit the growth of Plasmodium spp. Fosmidomycin [(3-(N-hydroxyformamido)propyl)phosphonic acid, 1] and its acetyl homologue FR-900098 [(3-(N-hydroxyacetamido)propyl)phosphonic acid, 2] potently inhibit 1-deoxy-d-xylulose-5-phosphate reductoisomerase (Dxr), a key enzyme in this biosynthetic pathway. Arylpropyl substituents were introduced at the β-position of the hydroxamate analogue of 2 to study changes in lipophilicity, as well as electronic and steric properties. The potency of several new compounds on the P. falciparum enzyme approaches that of 1 and 2. Activities against the enzyme and parasite correlate well, supporting the mode of action. Seven X-ray structures show that all of the new arylpropyl substituents displace a key tryptophan residue of the active-site flap, which had made favorable interactions with 1 and 2. Plasticity of the flap allows substituents to be accommodated in many ways; in most cases, the flap is largely disordered. Compounds can be separated into two classes based on whether the substituent on the aromatic ring is at the meta or para position. Generally, meta-substituted compounds are better inhibitors, and in both classes, smaller size is linked to better potency.

Metal-Free Enantioselective Oxidative Arylation of Alkenes: Hypervalent-Iodine-Promoted Oxidative C?C Bond Formation

The enantioselective oxyarylation of (E)-6-aryl-1-silyloxylhex-3-ene was achieved using a lactate-based chiral hypervalent iodine(III) reagent in the presence of boron trifluoride diethyl etherate. The silyl ether promotes the oxidative cyclization, and enhances the enantioselectivity. In addition, the corresponding aminoarylation was achieved.

Iron-catalyzed arene alkylation reactions with unactivated secondary alcohols

A simple, iron-based catalytic system allows for the inter- and intramolecular arylation of unactivated secondary alcohols. This transformation expands the substrate scope beyond the previously required activated alcohols and proceeds under mild reaction conditions, tolerating air and moisture. Furthermore, the use of an enantioenriched secondary alcohol provides an enantioenriched product for the intramolecular reaction, thereby offering a convenient approach to nonracemic products.

Structural optimization of 4-(2-chlorophenyl)-9-methyl-6H-thieno [3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines as antagonists for platelet activating factor: Pharmacological contribution of substituents at the 2- and 6-positions of a condensed ring system

A series of 4-(2-chlorophenyl)-9-methyl-6H-thieno [3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives bearing substituents at the 2- and 6-positions were synthesized, and evaluated in vitro for their inhibitory activity on rabbit platelet aggregation induced by platelet activating factor (PAF) and in vivo for their preventing effect on PAF-induced mortality in mice. The length of alkyl or arylalkyl side chain at the 2-position was responsible for enhancing the affinity for the PAF receptor. The simultaneous substitution at both the 2- and 6-positions resulted in a successful separation of the affinity for the PAF receptor from that for the benzodiazepine (BZ) receptor. Thus, (±)-4-(2-chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]- 6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4] diazepine (Y-24180) was confirmed to be a specific antagonist for the PAF receptor and is currently under clinical trials.