Claims
- 1. A compound of the formula ##STR5## wherein n is the integer 0, 1 or 2; each X independently is a substituent selected from the group consisting of loweralkyl, halo, --O--(loweralkyl), --S--(loweralkyl), --SO--(loweralkyl), --SO.sub.2 --(loweralkyl), CO.sub.2 R and CH.sub.2 OR, wherein R is loweralkyl and each loweralkyl group is from 1 to about 6 carbon atoms, or a pharmaceutically acceptable addition salt thereof.
- 2. A compound of claim 1 wherein n is 0.
- 3. A compound of claim 1 wherein n is 1.
- 4. A compound of claim 3 wherein X is selected from the group consisting of halo and loweralkyl.
- 5. A compound of claim 3 wherein X is --O-- or --S-- (loweralkyl).
- 6. A compound of claim 3 wherein X is CO.sub.2 R.
- 7. The compounds of claim 3 wherein X is CH.sub.2 OR.
- 8. A compound of claim 3 wherein X is loweralkyl of from 1 to about 4 carbon atoms.
- 9. A process for preparing a compound of the formula ##STR6## wherein n is the integer 0, 1 or 2; each X independently is a substituent selected from the group consisting of loweralkyl, halo, --O--(loweralkyl), --S--(loweralkyl, --SO--(loweralkyl), ---SO.sub.2 --(loweralkyl), CO.sub.2 R and CH.sub.2 OR, wherein R is loweralkyl and each loweralkyl group is from 1 to about 6 carbon atoms, or a pharmaceutically acceptable addition salt thereof which comprises reacting a protected amine compound of the formula:
- R'CH.sub.2 C.tbd.CCH.sub.2 N(SiMe.sub.3).sub.2
- with a metallo-organic compound of the formula ##STR7## wherein X and n are as above defined, R' is alkoxy of from 1 to 4 carbon atoms, and M is an organometallo reagent, in the presence of an inert solvent and a nickel catalyst, and further treating the resulting product bearing a silyl protected amine group with a deprotecting agent to obtain the desired compound.
- 10. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable addition salt thereof, in combination with a pharmaceutically acceptable carrier.
- 11. A method of treating hypertension in a mammal in need thereof which comprises administering to said mammal an antihypertensive effective amount of a compound of claim 1, or a pharmaceutically acceptable addition salt thereof.
CROSS-REFERENCE TO RELATED APPLICATION
This is a division of application Ser. No. 153,106 filed Feb. 8, 1988, now U.S. Pat. No. 4,847,288, which is a continuation-in-part of application Ser. No. 945,460, filed Dec. 23, 1986, now abandoned.
US Referenced Citations (5)
Non-Patent Literature Citations (2)
Entry |
Claesson, A., and Sahlberg, C., Tetrahedron, 38(3), 363-8 (1982). |
Sahlberg, C., Svante, B. R. Fagewall, I., Ask, A., and Claesson, A., J. Med. Chem. 26(7), 1036-42 (1983). |
Divisions (1)
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Number |
Date |
Country |
Parent |
153106 |
Feb 1988 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
945460 |
Dec 1986 |
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