Indole, azaindole and related heterocyclic N-substituted piperazine derivatives
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Example
Preparation of Example 1 from PCT / US02 / 00455
Typical Boron / palladium coupling procedure
can be used as a procedure for
or even as a procedure for
where Rx is as described for Scheme 6B
Example
Preparation of Example 39 from PCT / US02 / 00455
An example of the typical stannane / palladium coupling procedure
can be used as a procedure for
or even as a procedure for
where Rx is as described for Scheme 6B
Example
Preparation of Example 20 from PCT / US01 / 20300
An example to show how functionalization procedures of oxoacetyl piperazine benzamides can be used to carry out similar tranformations in the corresponding piperidine alkenes
can be used as a procedure for
or even as a procedure for
where Rx is as described for Scheme 6B
Preparation of Intermediates and Examples:
All starting materials, unless otherwise indicated can be purchased from commercial sources. Methods are given for the preparation of intermediates.
Note: Unless Otherwise indicated, HPLC conditions utilized column G.
To a mixture of 1-chloroisoquinoline (527 mg, 3.22 mmol) and tert-butyl 1-piperazinecarboxylate (500 mg, 2.68 mmol) in ethylene glycol (8 ml) at r.t. was added triethylamine (2.0 ml, 14.3 mmol). The reaction mixture was then stirred at 100° C. for 6 to 20 h. After cooling to r.t., the mixture was diluted with water (30 ml), basified using saturated aqueous NaHCO3, and extracted with CH2Cl2 (50 ml). The...
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