65340-85-4

Upstream product

• 306-08-1 Homovanillic acid 
• 100-39-0 benzyl bromide 
• 100-44-7 benzyl chloride 

Downstream Products

• 56355-43-2 4-hydroxy-3-methoxy-phenylpropionic acid 
• 1391847-92-9 C₂₁H₂₇NO₃ 
• 1391848-04-6 C₂₁H₂₇NO₃ 
• 1391847-90-7 C₁₈H₂₉NO₃ 
• 1391847-91-8 C₁₉H₃₁NO₃ 
• 1391847-85-0 C₂₄H₂₄O₄ 
• 64881-05-6 1-<4-(benzyloxy)-3-methoxyphenyl>ethan-2-ol 
• 1454883-54-5 7-(benzyloxy)-1-((6-bromobenzo[d][1,3]dioxol-5-yl)methyl)-6-methoxyisochroman 
• 1454883-55-6 1-(benzyloxy)-2-methoxy-4,5,6a,7-tetrahydro-[1,3]dioxolo[4',5':4,5]benzo[1,2-g]benzo[de]chromene 
• 788110-09-8 2-benzylamino-6-hydroxy-7-methoxy-1,2,3,4-tetrahydronaphthalene 
• 75236-17-8 2-amino-6-hydroxy-7-methoxy-1,2,3,4-tetrahydronaphthalene 
• 54313-35-8 2-(4-(benzyloxy)-3-methoxyphenyl)acetyl chloride 
• 29973-91-9 4-benzyloxy-3-methoxyphenylacetic acid 

Relevant academic research and scientific papers

Preparation method for ivabradine impurities

The invention discloses a preparation method for ivabradine impurities. According to the preparation method, 3-hydroxy-4-methoxyphenylacetic acid (as shown in a formula 1a) and 4-hydroxy-3-methoxyphenylacetic acid (as shown in a formula 1b) are respectively used as a starting raw material and subjected to multiple steps of reactions to prepare two impurities of ivabradine. The preparation method of the invention is simple and realizes high-purity preparation; and the prepared impurities can be used for qualitative and quantitative analysis so as to improve the medication safety of ivabradine.

Interrupted Pummerer Reaction in Latent-Active Glycosylation: Glycosyl Donors with a Recyclable and Regenerative Leaving Group

Latent O-glycosides, 2-(2-propylthiol)benzyl (PTB) glycosides, were converted into the corresponding active glycosyl donors, 2-(2-propylsulfinyl)benzyl (PSB) glycosides, by a simple and efficient oxidation. Treatment of the PSB donor and various acceptors with triflic anhydride provided the desired glycosides in good to excellent yields. The leaving group, which was activated by an interrupted Pummerer reaction, can be recycled (PSB-OH) and regenerated as the precursor (PTB-OH). A natural hepatoprotective glycoside, leonoside F, was efficiently synthesized in a convergent [3+1] manner with this newly developed method. The present total synthesis also led to a structural revision of this phenylethanoid glycoside.

Facile synthesis of 4,5,6a,7-tetrahydrodibenzo[de,g]chromene heterocycles and their transformation to phenanthrene alkaloids

Oxa-Pictet-Spengler cyclization and microwave-assisted C-H arylation have been implemented as key steps in the synthesis of new isochroman heterocycles containing a 4,5,6a,7-tetrahydrodibenzo[de,g]chromene motif. These isochromans may be easily transformed to phenanthrene alkaloids via acidic cleavage of the isochroman ring and standard synthetic manipulations thereafter. The route described is attractive in that it provides access to two biologically interesting scaffolds in simple and high yielding synthetic steps.

The SAR analysis of TRPV1 agonists with the α-methylated B-region

A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogues were investigated. Whereas the α-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The analysis indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.

AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS

There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.