1261352-32-2

Upstream product

• 3040-44-6 1-piperidinoethanol 
• 1135317-03-1 3-(4-hydroxyphenyl)-5-methoxy-2-(4-methoxyphenyl)benzo[b]thiophene 
• 1163701-04-9 4-methoxy-2-[ (4-methoxyphenyl)ethynyl]thioanisole 
• 1163701-64-1 C₂₇H₂₆O₄S 
• 4897-68-1 2-iodo-4-methoxybromobenzene 
• 149457-46-5 4-bromo-3-[(4-methoxyphenyl)ethynyl]anisole 
• 768-60-5 4-methoxyphenylacetylen 
• 334708-34-8 3-iodo-5-methoxy-2-(4-methoxyphenyl)benzo[b]thiophene 

Downstream Products

• 1261352-37-7 C₂₇H₂₇NO₃S 

Relevant academic research and scientific papers

Parallel synthesis of a desketoraloxifene analogue library via iodocyclization/palladium-catalyzed coupling

For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic amine side chain. This approach affords oxygen-bearing 3-iodobenzo[b]thiophenes 4 in excellent yields, which are easily further elaborated using a two-step approach involving Suzuki-Miyaura and Mitsunobu coupling reactions to give multimethoxy-substituted desketoraloxifene analogues 6. Various hydroxyl-substituted desketoraloxifene analogues 7 were subsequently generated by demethylation with BBr3.

A new approach to desketoraloxifene analogs from oxygen-bearing 3-iodobenzo[b]thiophenes prepared via iodocyclization

A formal total synthesis of the benzothiophene selective estrogen receptor modulator (SERM) desketoraloxifene and analogs has been accomplished from alkynes bearing electron-rich aromatic rings by electrophilic cyclization using I2. This approa