# US 5,710,285 A · Process for preparing 2-substituted benzo›B!thiophene compounds and intermediates thereof

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- Number: US 5,710,285 A
- Document ID: US5710285A
- Status: Granted
- Kind: A
- Application number: 08/549,595
- Filed: 1995-10-27
- Granted: 1998-01-20
- Earliest claimed: 1995-03-31
- Assignees: Eli Lilly and Company
- Inventors: Kenneth L. Hauser; Alan D. Palkowitz; Daniel J. Sall; Kenneth J. Thrasher
- Web page: https://patentgrep.com/patent/US5710285A

## CPC

- C07D 333/54: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D 333/56: Radicals substituted by oxygen atoms
- C07D 333/62: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07F 5/025: {Boronic and borinic acid compounds}
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

The present invention provides useful intermediates for preparing 2-(substituted phenyl)benzothiophenes compounds said intermediates having the structure ##STR1## wherein R.sup.1 ' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; and Z is bromo, iodo, triflate, or --B(OH).sub.2 with the proviso that when Z is bromo or iodo, R1' is not alkoxy.

## Claims

### Claim 1

A compound of formula IX ##STR24## wherein R.sup.1 IS --OH or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; and
Z is bromo, iodo, triflate or --B(OH).sub.2 ;
with the proviso that when Z is bromo or iodo, R.sup.1 ' is not alkoxy.

### Claim 2 (depends on 1)

A compound according to claim 1 wherein R.sup.1 ' is --OR.sup.3.

### Claim 3 (depends on 2)

A compound according to claim 2 wherein R.sup.3 is C.sub.1 -C.sub.4 alkyl.

### Claim 4 (depends on 3)

A compound according to claim 3 wherein R.sup.3 is methyl.

### Claim 5 (depends on 4)

A compound according to claim 4 wherein Z is --B(OH).sub.2.

### Claim 6 (depends on 1)

A compound according to claim 1 wherein Z is bromo.

### Claim 7 (depends on 1)

A compound according to claim 1 wherein Z is iodo.

### Claim 8 (depends on 1)

A compound according to claim 1 wherein Z is --B(OH).sub.2.