Process for the preparation of 4 - ((4 - ((4 - (2 - cianoetenil) - (2,6-dimethylphenyl) amino) - 2 - pirimidinil) amino) benzonitrile, processes for the preparation of an intermediary, and Compound 4 - ((4 - ((4 - (2 - cianoetenil) - 2.6 - dimetilfenil) amino) - 2 - pirimidinil) amino) benzonitrile

摘要

1. Formula of 4 - [[4 - [[4 - (2-cyano-phenyl) - 2, 6-Dimethylphenyl] - amino] - 2-pyridine] amino] benzo-p-dioxin (1),Nitrous oxide, a pharmaceutically acceptable acid addition salt, a tetraacetamide or its stereochemical isomerization form, including: (a) reacting the preparation intermediate (2),A suitable acid salt or a three-dimensional form of salt similar to the chemical plasma and a formula medium (3),An appropriate acid salt or nitrous oxide, wherein W1 represents an appropriate emission group, there is an appropriate solvent, and free radicals can be converted into an added acid salt through acid treatment as appropriate, or vice versa, The acid salt additive form is converted to free radicals by alkali treatment; if necessary, it can also be selected to be followed by the preparation of stereoisomerization form, nitrogen oxide form or quadrilateral amine; (b) the preparation intermediate reacts (4),A suitable acid salt or positive oxide salt, wherein W2 represents an appropriate discharge group, acrylonitrile and a suitable paladio catalyst, a suitable substrate and a suitable solvent, and if necessary, the free radical can be converted into an added acid salt by the following treatment: An acid, or vice versa, that converts the form of an acid salt additive to a free base by alkali treatment; or, optionally, subsequently by manufacturing a stereochemical isomerization form, a nitrous oxide form, or tetrachloroaniline; or (c) reacting a formula intermediate (5),An appropriate acid salt or an acid salt in the same three-dimensional form as the chemical plasma, with a preparation medium (3),A suitable acid salt or nitrous oxide, wherein W1 represents a suitable discharge group, with a suitable solvent, and then dehydrated with the obtained formula intermediate (6), an acceptable salt added with a medicament, 1. In the form of stereoisomerization isomer or positive oxide, if necessary, the base can be changed to acid salt or vice versa; You can choose if you likea. To produce its chemical isomerization stereoscopic form, nitrogen oxide form or quadrilateral amine; or (d) to make the prepared intermediate react (4),A suitable acid salt or positive oxide salt, wherein W2 represents a suitable throwing group, acrylamide with proper polishing catalyst, proper base and solvent, and then dehydrated by the obtained formula intermediate (6), A pharmaceutically acceptable acid salt, a stereoisomerized isomerized or nitrous oxide form, which, if necessary, can be converted into an acid salt by acid treatment, or vice versa, 1. Through alkali treatment, the form of acid salt additive is transformed into open-air base;If necessary, it can also choose to use its stereoisomerization isomerization form, oxide or quadrilateral amine. Procedures for the development of a formula intermediary (2) have also been published.Acid salt, tetraacetamide or appropriate stereoisomer forms, including: (1) preparation medium reaction (7),3. An appropriate acid salt or tetrachloroaniline, wherein W3 represents an appropriate throw group, acrylonitrile is equipped with an appropriate paladi catalyst, an appropriate base and a suitable solvent, and if necessary, it can be chosen to follow closely; The form of an acid salt additive is converted to an added acid salt by acid treatment or, conversely, by alkali treatment; if necessary, it can then be formulated in a stereoisomeric form, a. In the form of nitrous oxide or quadrilateral amine;o. (II) to make the preparation intermediary react (7);An appropriate acid salt or quaternary amine, wherein W3 represents an appropriate throwing group, acrylonitrile has an appropriate shovel catalyst, a suitable base and a solvent, and then the formula intermediate is dehydrated (5), obtained in this way, The addition of acid salts, tetrachloroaniline or the same suitable form of stereochemical isomerization, with the option of converting free radicals to added acid salts by acid treatment, if necessary, or vice versa,Through alkali treatment, the form of acid salt additive can be transformed into free radicals; if necessary, it can also be transformed into free radicals through the preparation of chemical isomerization stereoscopic form, nitrous oxide or quadrilateral amine. In addition, 4 - [[4 - [[4 - (2-cyano-phenyl) - 2,6-Dimethylphenyl] - amino] - 2-pyridyl-amino] benzodiazepine] formula (1) was also published,Its N-oxide, acceptable acid additive salt, tetraacetamide and stereoisomer. The above compounds (fla.i) have the activity of inhibiting H.I.V. replication.