- Diamine as well as preparation method and application thereof (by machine translation)
-
The structural formula of the diamine is shown as a formula (I). The invention also discloses a preparation method of the diamine, which comprises the following steps: 2 - chlorine -5 - bromobenzoate and magnesium metal; a metallization reaction occurs un
- -
-
Paragraph 0042-0043; 0045
(2020/12/31)
-
- Synthesis and bioactivity of sulfide derivatives containing 1,3,4-oxadiazole and pyridine
-
A series of novel sulfide derivatives containing 1,3,4-oxadiazole and pyridine were synthesized, characterized, and tested for their antibacterial activity against tobacco bacterial wilt and rice bacterial blight and for insecticidal activity toward diamondback moth. The results showed that some compounds had good insecticidal and bactericidal activity, e.g., the activities of compounds 6e and 6g–6j toward tobacco bacterial wilt were much better than those of commercial thiodiazole-copper, and some of the synthesized compounds possessed good insecticidal activity against Plutella xylostella. Compounds 6d, 6h, 6j, 6l, 6p, 6r, and 6p displayed over 93% activity at 500 mg L? 1.
- Yu, Gang,Chen, Shunhong,He, Feng,Luo, Dexia,Zhang, Yu,Wu, Jian
-
p. 1075 - 1085
(2019/09/10)
-
- Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety
-
A series of trifluoromethyl pyridine derivatives containing 1,3,4-oxadiazole moiety was designed, synthesized and bio-assayed for their insecticidal activity. The result of bio-assays indicated the synthesized compounds exhibited good insecticidal activity against Mythimna separata and Plutella xylostella, most of the title compounds show 100% insecticidal activity at 500 mg L-1 and >80% activity at 250 mg L-1 against the two pests. Compounds E18 and E27 showed LC50 values of 38.5 and 30.8 mg L-1 against Mythimna separata, respectively, which were close to that of avermectin (29.6 mg L-1); compounds E5, E6, E9, E10, E15, E25, E26, and E27 showed 100% activity at 250 mg L-1, which were better than chlorpyrifos (87%). CoMFA and CoMSIA models with good predictability were proposed, which revealed the electron-withdrawing groups with an appropriate bulk at 2- and 4-positions of benzene ring could enhance insecticidal activity.
- Xu,Wang,Luo,Yu,Guo,Fu,Zhao,Wu
-
p. 6306 - 6314
(2018/02/19)
-
- 4-METHYL-2,3,5,9,9B-PENTAAZA-CYCLOPENTA[A]NAPHTHALENES
-
The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
- -
-
Page/Page column 95-97
(2014/02/16)
-
- 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
-
The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
- -
-
Paragraph 0565-0568; 0577
(2014/03/21)
-
- Regio- and chemoselective C-H chlorination/bromination of electron-deficient arenes by weak coordination and study of relative directing-group abilities
-
It's all relative: A practical and efficient PdII-catalyzed regio- and chemoselective chlorination/bromination has been developed for the facile synthesis of a broad range of aromatic chlorides. The reaction demonstrates excellent reactivity, good functional-group tolerance, and high yields. A preliminary study was conducted to evaluate relative directing-group abilities of various functionalities. Copyright
- Sun, Xiuyun,Shan, Gang,Sun, Yonghui,Rao, Yu
-
supporting information
p. 4440 - 4444
(2013/05/22)
-
- Gem-dimethyl-bearing C-glucosides as sodium-glucose co-transporter 2 (SGLT2) inhibitors
-
Three novel gem-dimethyl C-glucosides were designed as sodium-glucose co-transporter 2 (SGLT2) inhibitors, and their syntheses started from D-glucose and three 2-substituted-5-bromobenzoic acids were achieved via a facile 8-step protocol, with the key step being anhydrous aluminum chloride-catalyzed Friedel-Crafts alkylation of tertiary alcohols and phenetol. These three SGLT2 inhibitors were evaluated in vivo with a mice oral glucose tolerance test (OGTT), and the anti-hyperglycemic activities of all these three compounds were comparable with that of the positive control Dapagliflozin. Copyright
- Shi, Yongheng,Zhao, Guilong,Lou, Yuanyuan,Wang, Yuli,Shao, Hua,Liu, Wei,Xu, Weiren,Tang, Lida
-
experimental part
p. 1192 - 1198
(2012/04/23)
-
- Use of Potassium Bromate: Bromination of Halobenzenes and Halobenzoic Acids
-
Syntheses of bromo compounds by the bromination of halobenzenes and halobenzoic acids using potassium bromate under acidic condition have been discussed.
- Banerjee, Amalendu,Banerjee, Gopal Chandra,Dutt, Sachchidananda,Banerjee, Santa (Mrs.),Samaddar, Haraprasad
-
p. 640 - 642
(2007/10/02)
-