Claims
- 1. A method of preparing a compound of the formula, ##STR25## where Y is hydrogen, fluorine, chlorine, bromine, nitro, loweralkyl, loweralkoxy or triloweralkylsilyl;
- R.sub.1 is loweralkyl, halogen-substituted loweralkyl, aryl, arylloweralkyl, cycloalkyl having from 3 to 7 carbon atoms in the ring, heteroaryl or heteroarylloweralkyl;
- R.sub.2 is loweralkyl or arylloweralkyl;
- R.sub.3 is loweralkyl or arylloweralkyl;
- R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl;
- R.sub.5 is hydrogen or loweralkyl;
- wherein the term heteroaryl signifies a group depicted by the formula ##STR26## where R.sub.6 is hydrogen or loweralkyl; which comprises reacting a compound of the formula, ##STR27## with a strong base and allowing the resultant anion to react with a compound of the formula R.sub.2 --Cl or R.sub.2 --Br to afford said compound.
- 2. A method of preparing a compound of the formula, ##STR28## where R.sub.1 is loweralkyl, halogen-substituted loweralkyl, aryl, arylloweralkyl, cycloalkyl having from 3 to 7 carbon atoms in the ring, heteroaryl or heteroarylloweralkyl;
- R.sub.2 is loweralkyl or arylloweralkyl;
- R.sub.3 is loweralkyl or arylloweralkyl;
- R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl;
- R.sub.5 is hydrogen or loweralkyl;
- X' is oxygen or sulfur; and
- Y is hydrogen, fluorine, chlorine, bromine, nitro, loweralkyl, loweralkoxy or triloweralkylsilyl;
- wherein the term heteroaryl signifies a group depicted by the formula ##STR29## where R.sub.6 is hydrogen or loweralkyl; which comprises reacting a compound of the formula, ##STR30## and thereafter reacting the resultant anion with a disulfate compound of the formula R.sub.2 --O--SO.sub.2 --O--R.sub.2 or a mesylate of the formula R.sub.2 O--SO.sub.2 --CH.sub.3 or a chloride or bromide of the formula R.sub.2 Cl or R.sub.2 Br to afford said compound.
- 3. A method of preparing a compound of the formula, ##STR31## where R.sub.1 is loweralkyl, halogen-substituted loweralkyl, aryl, arylloweralkyl, cycloalkyl having from 3 to 7 carbon atoms in the ring, heteroaryl or heteroarylloweralkyl;
- R.sub.2 is loweralkyl or arylloweralkyl;
- R.sub.3 is loweralkyl or arylloweralkyl;
- R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl;
- R.sub.5 is hydrogen or loweralkyl; and
- Y is hydrogen, fluorine, chlorine, bromine, nitro, loweralkyl, loweralkoxy or triloweralkylsilyl;
- wherein the term heteroaryl signifies a group depicted by the formula ##STR32## where R.sub.6 is hydrogen or loweralkyl; which comprises converting a compound of the formula, ##STR33## to an amine compound of the formula, ##STR34## by heating at a temperature of about 150.degree.-250.degree. C. in the absence of base and thereafter allowing the latter compound to react with an isocyanate of the formula R.sub.1 NCO to afford said compound.
- 4. The method of claim 1 wherein the strong base is sec-BuLi.
Parent Case Info
This is a division of a prior application Ser. No. 480,706, filed Feb. 1, 1990, now U.S. Pat. No. 4,983,616.
Non-Patent Literature Citations (1)
Entry |
March, Advanced Organic Chemistry, 3rd Edition, pp. 338-341; 364-365; 577; 802-83; 310-313 (1985). |
Divisions (1)
|
Number |
Date |
Country |
Parent |
480706 |
Feb 1990 |
|