C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/253, 260/265
C07D 403/12 (2006.01) A61K 31/495 (2006.01) C07D 233/44 (2006.01) C07D 239/72 (2006.01) C07D 241/42 (2006.01) C07D 401/12 (2006.01) C07D 233/48 (2006.01) C07D 241/44 (2006.01)
Patent
CA 1043791
ABSTRACT OF THE DISCLOSURE This invention relates to a process for preparing derivatives of quinoxaline and quinazoline which are described and claimed in British Patent No. 1,381,979. According to the invention there is provided an improved process for preparing a compound of the formula: Image (I) where Q represents a group of the formula: Image or Image in which the free valence may be in any one of the 5-, 6-, 7- or 8-positions in the quinoxaline or quinazoline nucleus; (R1)x represents up to 3 optional substituents in any of the remaining 5-, 6-, 7- or 8-positions, each R1 being a halogen atom or a lower alkyl, lower alkoxy or trifluoromethyl group and x being 0 to 3; and R2 represents an optional substituent in either of the 2- or 3-, or 2- or 4-positions of the quin- oxaline or quinazoline nucleus, respectively, R2 being a hydrogen atom or a lower alkyl or lower alkoxy group; by reacting the corresponding isothiocyanate of the formula Q-NCS, with ethylene diamine to form a .beta.-aminoethyl thio- ureido compound of the formula Q-NH.CS.NHCH2CH2NH2, cyclizing the .beta.-aminoethyl-thioureido compound to form the compound of the formula (I), recovering the latter as the product, and optionally, converting the product into a pharmaceutically acceptable acid addition salt, the improvement which comprises preparing said isothiocyanate by heating a thiouraido compound of the formula Q-NHCSNH2, wherein Q is as defined above.
234270
Thomas Michael B.
Williams Michael T.
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