- A convenient synthesis of new annelated pyrimidines and their biological importance
-
Several bicyclic/tricyclic-fused pyrimidines were synthesized from the reactions of amino esters and bifunctional nucleophiles such as 2-methylthio-thiazoline and 2-methylthio-imidazoline. The synthesized compounds were tested for their in vitro antimicrobial activities that revealed mild to moderate growth inhibitory potentials.
- Wahab Khan,Uddin, Mohammed Kabir,Ali, Morshed,Rahman, Mohammad S.,Rashid, Mohammad Abdur,Chowdhury, Rasheduzzaman
-
-
Read Online
- N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
-
The invention relates to compounds of formula (I), or a salt thereof wherein R1, A, L, and R2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are ανβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.
- -
-
Paragraph 0506
(2018/03/28)
-
- Method for synthetizing Tebipenem intermediate
-
The invention discloses a method for synthetizing a Tebipenem intermediate, and belongs to the field of chemical pharmacy. 2- methylthio-4, 5- thiazoline is synthetized by using ethanolamine as a raw material, a disulfide bond and a C-N coupling and breaking disulfide bond are formed through addition, cyclization, open loop and hydrolysis by using allyl amine as a raw material, and finally the Tebipenem intermediate namely 1- ( 4,5- thiazoline -2- base) azetidine -3- mercaptide hydrochloride is synthetized. The method disclosed by the invention is simple and easy to operate, high in yield, low in pollution and suitable for industrial production.
- -
-
Paragraph 0006; 0007
(2016/11/28)
-
- S-methylation of N-containing heterocyclic thiols with conjugated acids of methoxy groups
-
2-Mercaptopyridine-3-carboxylic acid reacts with methanol under acidic conditions to afford the corresponding S-methylated methyl ester, methyl 2-methylthiopyridine-2-carboxylate. Such S-methylation occurred for various N-containing heterocyclic thiols wi
- Shimizu, Masao,Shimazaki, Teruaki,Kon, Yoshihiro,Konakahara, Takeo
-
experimental part
p. 413 - 420
(2010/09/05)
-
- 4,5-Dihydrothiazoline - A new protecting and activating group for generation of α-aminocarbanions of secondary amines
-
4,5-Dihydrothiazoline has been successfully used as a protecting and activating group for synthesis of various 1-substituted 1,2,3,4- tetrahydroisoquinolines via a lithiation-electrophillic substitution reaction sequence. Copyright Taylor & Francis Group, LLC.
- Singh, Kamal Nain,Singh, Paramjit,Kaur, Amarjit
-
p. 3339 - 3343
(2007/10/03)
-
- Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase
-
Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.
- Shankaran,Donnelly, Karla L.,Shah, Shrenik K.,Guthikonda, Ravindra N.,MacCoss, Malcolm,Humes, John L.,Pacholok, Stephen G.,Grant, Stephan K.,Kelly,Wong
-
p. 4539 - 4544
(2007/10/03)
-
- Formation and Rearrangement of Cyclic Semi-aminals with α-Mercapto Groups
-
Reaction of thioacetic acid, thiobenzoic acid as well as 2-aminothiophenol with racemic cyclic semi-aminal 3 takes a diastereoselective course to racemic 4a, b, c.The ambident thiazolidine-2-thione reacts analogously, however by attack of nitrogen yielding 4d.The possibilities for rearrangement of adducts 4 are discussed and the structure of the rearranged products is examinated by x-ray analysis of 9c as well as by 13C NMR spectroscopy.The course of the diastereoselective rearrangement to the racemic mixture (α/β) of 2-azaspirononenes 9a-d is discussed by aid of the results.
- Kucklaender, Uwe,Edoho, Edoho J.,Rinus, Olaf,Massa, Werner
-
p. 3405 - 3415
(2007/10/02)
-