104202-36-0

Upstream product

• 104202-49-5 3-Methoxy-4-methoxymethoxyphenol 
• 77-78-1 dimethyl sulfate 
• 13330-65-9 2,4-dimethoxyphenol 
• 107-30-2 chloromethyl methyl ether 
• 121-33-5 vanillin 
• 5533-00-6 3-methoxy-4-methoxymethoxy-benzaldehyde 
• 613-45-6 2,4-Dimethoxybenzaldehyde 

Downstream Products

• 2880-58-2 2-methoxy-1,4-benzoquinone 
• 622347-41-5 2,6-dimethoxy-3-methoxymethoxy-benzaldehyde 
• 232275-39-7 2,6-Dimethoxy-3-methoxymethoxybenzeneboronic acid 
• 622347-38-0 (2E)-2-methyl-but-2-enoic acid {3-[(4R)-4-(tert-butyl-dimethyl-silanyloxy)-(2R)-2-methylheptyl]-2,4-dimethoxy-5-methoxymethoxy-phenyl}amide 
• 622347-34-6 (4S)-4-benzyl-3-[3-(2,6-dimethoxy-3-methoxymethoxy-5-nitro-phenyl)-(2R)-2-methylpropionyl]-oxazolidin-2-one 
• 622347-45-9 tert-butyl-{(1R)-1-[3-(2,6-dimethoxy-3-methoxymethoxy-5-nitro-phenyl)-(2R)-2-methylpropyl]-but-3-enyloxy}dimethylsilane 
• 622347-46-0 3-[(4R)-4-(tert-butyl-dimethyl-silanyloxy)-(2R)-2-methylheptyl]-2,4-dimethoxy-5-methoxymethoxy-phenylamine 
• 622347-39-1 2-methyl-but-(2E)-2-enoic acid [(5-hydroxy-3-(4R)-4-hydroxy-(2R)-2-methylheptyl)-2,4-dimethoxy-5-methoxymethoxy-phenyl]amide 
• 622347-43-7 4-(2,6-dimethoxy-3-methoxymethoxy-5-nitro-phenyl)-(3R)-3-methylbutyronitrile 
• 622347-44-8 4-(2,6-dimethoxy-3-methoxymethoxy-5-nitro-phenyl)-(3R)-3-methylbutyraldehyde 
• 622347-36-8 3-(2,6-dimethoxy-3-methoxymethoxy-5-nitro-phenyl)-(2R)-2-methylpropan-1-ol 
• 622347-35-7 3-bromomethyl-2,4-dimethoxy-1-methoxymethoxy-5-nitrobenzene 
• 622347-42-6 (2,6-dimethoxy-3-methoxymethoxy-5-nitro)benzyl alcohol 
• 622347-33-5 2,6-dimethoxy-3-methoxymethoxy-5-nitro-benzaldehyde 

Relevant academic research and scientific papers

Selective Synthesis of the para-Quinone Region of Geldanamycin

(Matrix presented) The quinone portion of the ansamycin geldanamycin was made with complete selectivity from the 1,4-dihydroquinone generated from a 1,4-bis-methoxymethyl (MOM) ether intermediate. Palladium catalysis with air gave the desired product in 9

Inhibitors of α4 mediated cell adhesion

The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O-(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur, W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2and R3are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4is tetrazolyl, carboxyl group, amide or ester; R5is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl etc.; R6is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.; or a pharmaceutically acceptable salt thereof.

Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: Discovery of TR-14035, a dual α4β7/α4β1 integrin antagonist

α4β1 and α4β7 integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of anti-integrin antibodies to attenuate a number of inflammatory/immune conditions provides a strong rationale to target integrins for drug development. Important advances have been made in identifying potent and selective candidates, peptides and peptidomimetics, for further development. Herein, we report the discovery of a series of novel N-benzoyl-L-biphenylalanine derivatives that are potent inhibitors of α4 integrins. The potency of the initial lead compound (1: IC50 α4β7/α4β1 =5/33 μM) was optimized via sequential manipulation of substituents to generate low nM, orally bioavailable dual α4β1/α4β7 antagonists. The SAR also led to the identification of several subnanomolar antagonists (134, 142, and 143). Compound 81 (TR-14035; IC50 α4β7/α4β1 =7/87 nM) has completed Phase I studies in Europe. The synthesis, SAR and biological evaluation of these compounds are described.

Phenol compound having antioxidative activity and the process for preparing the same

Disclosed are a phenol compound represented by the formula (1): STR1 wherein R0 represents H, alkyl or alkyloxy; R1 represents alkyl; R2 represents alkyl or alkyloxy; OR3 represents OH; R4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR7 ; where R7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): STR2 represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom, or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

An Improved Synthesis of 1,4-Benzo- and 1,4-Naphthoquinones Bearing Active Substituents

The synthesis of 1,4-benzoquinones and 1,4-naphthoquinones 3a-j carrying substituents such as methoxyl, allyl or oxiranyl was substantially improved.The 1-methoxy-4-methoxymethyloxy 2a-d, g-k or 1,4-bis(methoxymethyloxy) derivatives 2e-f were used, as a substrates instead of 1,4-dimethoxy derivatives 1a-j hitherto used and they were oxidized with silver(II) dipicolinate.Among numerous examples, the synthesis of a new analog of ubiquinone 3d with the oxiranyl substituent, being a new bioactivated alkylating agent, is reported.