Straightforward access to methyl-polyheterocycles from direct para-lithiation of 3-picoline
摘要:
Various heterocycles have been introduced on the 3-picoline nucleus via a regioselective BuLi-Me2N(CH2)(2)OLi (BuLi-LiDMAE) mediated para-lithiation. Useful methyl-polyheterocycles were efficiently prepared by a one-pot lithiation-stannylation-Stille coupling sequence. (C) 2001 Published by Elsevier Science Ltd.
LINCOSAMIDE DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
申请人:Umemura Eijirou
公开号:US20100184746A1
公开(公告)日:2010-07-22
An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R
1
represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R
1
represents aryl or a five- or six-membered monocyclic heterocyclic group; R
2
represents a hydrogen atom or C
1-6
alkyl; R
3
represents C
1-6
alkyl or C
3-6
cycloalkyl-C
1-4
alkyl; R
4
, R
5
, and R
6
represent a hydrogen atom; R
7
represents C
1-6
alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant
Streptococcus pneumoniae
. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
APPARATUS FOR SYNTHESIZING THE IMAGING AGENT 4-CHLORO-2-(1,1-DIMETHYLETHYL)-5-[[4-[[2-(FLUORO-[18F])ETHOXY]METHYL]PHENYL]METHOXY]-3(2H)-PYRIDAZINONE (FLUORPIRIDAZ [18F])
申请人:Lantheus Medical Imaging, Inc.
公开号:EP3653621A1
公开(公告)日:2020-05-20
An apparatus for synthesizing the imaging agent of the formula
comprising a cassette as shown in Figure 17 with a linear arrangement of a plurality of stopcock manifolds arranged in the order:
1) luer connections to gas inlet and [18O]H2O recovery;
2) anion exchange cartridge - column eluting solution;
3) spike connection for acetonitrile;
4) empty syringe;
5) reservoir with solution of imaging agent precursor;
6) reaction vessel;
7) outlet to HPLC;
8) syringe with solution of a stabilizing agent;
9) inlet from HPLC;
10) ethanol reservoir;
11) syringe with solution of a stabilizing agent;
12) syringe with water;
13) final product vial;
14) empty syringe; and
15) reaction vessel and exhaust;
further comprising tubing, an imaging agent synthesis module, wherein the apparatus is fluidically connected to the apparatus, and wherein the solution of a stabilizing agent comprises a solution comprising ascorbic acid or a salt thereof.
Straightforward access to methyl-polyheterocycles from direct para-lithiation of 3-picoline
作者:Julien Mathieu、Philippe Gros、Yves Fort
DOI:10.1016/s0040-4039(01)00033-8
日期:2001.3
Various heterocycles have been introduced on the 3-picoline nucleus via a regioselective BuLi-Me2N(CH2)(2)OLi (BuLi-LiDMAE) mediated para-lithiation. Useful methyl-polyheterocycles were efficiently prepared by a one-pot lithiation-stannylation-Stille coupling sequence. (C) 2001 Published by Elsevier Science Ltd.