4021-11-8Relevant articles and documents
Preparation method of 2-methylpyridine-4-formic acid
-
Paragraph 0062-0076, (2019/11/28)
The invention provides a preparation method of 2-methylpyridine-4-formic acid. The preparation method comprises the following steps: carrying out a substitution reaction on 4,4-dialkoxy butyronitrileor 4,4-dialkoxy butyrate (II) with chloroacetone, or carrying out a ring-opening addition reaction and oxidation reaction on 4,4-dialkoxy butyronitrile or 4,4-dialkoxybutyrate with propylene oxide toprepare 6,6-dialkoxy-4-cyano-n-hexyl-2-one or 6,6-dialkoxy-4-alkoxycarbonyl-n-hexyl-2-one (III); then carrying out a cyclization reaction with ammonia and ammonium salt; and finally carrying out an oxidation reaction and hydrolysis, and carrying out acidification by hydrochloric acid to prepare the 2-methylpyridine-4-formic acid (I). The method provided by the invention has mild conditions, concise process flow, and safe and simple operation; the generation amount of waste acid and waste water is small, greenness and environment friendliness are achieved; reaction selectivity is good; productcost is low; the yield and purity of the product are high; and green industrial production of 2-methylpyridine-4-formic acid and popularization of downstream products of 2-methylpyridine-4-formic acidare facilitated.
PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
-
Page/Page column 154, (2016/06/01)
The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
(AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AS INHIBITORS OF FIBRINOLYSIS
-
Page/Page column 61, (2015/05/26)
The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.