30058-79-8

Upstream product

• 45235-19-6 bis-(3,3-diethoxy-propyl)-sulfide 
• 79-00-5 1,1,2-trichloroethane 
• 107-02-8 acrolein 

Downstream Products

• 30251-94-6 5,6-dihydro-2H-thiopyran-3-carbaldehyde-(2,4-dinitro-phenylhydrazone) 
• 61571-06-0 tetrahydrothiopyran-3-carbaldehyde 

Relevant academic research and scientific papers

Preparation method of 3-formyl tetrahydrothiapyran compound

The invention discloses a preparation method of a 3-formyl tetrahydrothiapyran compound, and relates to the technical field of organic synthesis, and the preparation method comprises the following steps: (1) carrying out a heating reflux reaction on sodium sulfide and 2-(2-bromoethyl)-1, 3-dioxane as shown in a formula II to obtain bis (3, 3-dimethoxypropyl) sulfane; (2) under an acidic condition, carrying out a heating reflux cyclization reaction on the bis (3, 3-dimethoxypropyl) sulfane in the step (1) and sulfuric acid to obtain 3-formyl-5, 6-dihydrothiapyran as shown in a formula IV; and (3) in the presence of a catalyst, catalyzing the 3-formyl-5, 6-dihydrothiapyran as shown in the formula IV under high pressure to obtain the 3-formyl tetrahydrothiapyran compound as shown in the formula I. The method has the advantages that the raw materials are easy to obtain, the operation is simple, and the highest yield can reach 92%.

Derivatives of hexahydrobenzofuranone useful for the treatment of (inter alia) auto-immune or inflammatory disorders

Heterocyclic-substituted compounds of formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is - (CH2)n-; (a); (b), wherein R 10 is absent; or, (c) wherein R 3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tri-cyclic heteroaromatic group; B is -(CH 2 ) n3 -. wherein n 3 is 0-5, -CH 2 -O-, -CH 2 S-, -CH 2 -NR 6 -, -C(O)NR 6 -. -NR 6 C(O)-, (d), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR 6 - when the double dotted line represents a single bond, or X is H, -OH or -NHR 20 when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C 1 -C 6 alkoxy) when the double dotted line represents a single bond or when the bond is absent, Y is =O, =NOR 17 (H, H). (H, OH), (H, SH), (H, C 1 -C 6 alkoxy) or (H, substituted-amino); R 22 and R 23 are independently -OH, -OC(O)R 30 , OC(O)NR 30 R 31 , or optionally substituted alkyl, alkenyl, alkynyl, heterocycloalkyl, aryl, cycloalkyl, cycloalkenyl, carbonyl, amino, alkoxy, alkenyloxy, alkynyloxy, heterocycloalkyloxy, cycloalkyloxy, or cycloalkenyloxy; or R 22 and R 10 , or R 23 and R 11 , can form a carbocyclic or heterocyclic ring; and the remaining variables are as described in the specification, Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and blinders to cannabinoid receptors.

INDOLE CARBOXAMIDES AS IKK2 INHIBITORS

The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Process for the preparation of 5,6-dihydro-2H-thiopyran-3-carboxaldehyde derivatives wherein the reactions are conducted in a high boiling mineral oil without a catalyst

5,6-Dihydro-2H-thiopyran-3-carboxaldehydes of the formula STR1 where R denotes hydrogen or methyl, are prepared by a method in which acrolein or crotonaldehyde is reacted with hydrogen sulfide in a mineral oil whose boiling point is higher than those of the starting materials and of the end product, and the 5,6-dihydro-2H-thiopyran-3-carboxaldehyde is obtained by distillation. These aldehydes are important intermediates for the preparation of some crop protection agents.

Preparation of 3-formyltetrahydrothiopyrans

3-Formyltetrahydrothiopyrans are prepared by hydrogenating a 3-formyl-5,6-dihydro-2H-thiopyran in the presence of a catalyst containing nickel, cobalt, platinum, copper and/or silver; if necessary, the 3-formyl-5,6-dihydro-2H-thiopyrans are prepared by converting bis-(β-formylethyl) sulfides and/or 3-formyl-4-hydroxytetrahydrothiopyrans in the presence of an acidic catalyst, and, if required, these bis-(β-formylethyl) sulfides and/or 3-formyl-4-hydroxytetrahydrothiopyrans are prepared by reacting an acrolein with hydrogen sulfide (a) in the presence of a basic catalyst and of methylene chloride, aromatic hydrocarbons and/or 1,1,2-trichloroethane as solvents, and/or (b) in the presence of a carboxamide. The compounds obtainable by the process according to the invention are useful starting materials for the preparation of dyes, drugs and pesticides.