Syntheses of 1,2-di-O-palmitoyl-sn-glycero-3-phosphocholine (DPPC) and analogs with 13C- and 2H-labeled choline head groups
摘要:
The syntheses of four head group labeled analogs of 1,2-di-O-palmitoyl-sn-glycero-3-phosphocholine (DPPC) (6) by a general method from 1,2-di-O-palmitoyl-sn-glycero-3-phosphatidic acid (5) have been performed. The syntheses of 1,2-di-O-palmitoyl-sn-glycero-3-phospho[alpha-C-13]choline (6a) and 1,2-di-O-palmitoyl-sn-glycero-3-phospho[beta-C-13]choline (6b) were performed from labeled [1-C-13]glycine (1a) in 52% overall yield and from [2-C-13]glycine (1b) in 56%, overall yield, respectively. 1,2-Di-O-palmitoyl-sn-glycero-3-phospho[N((CH3)-H-2)(3)]choline (9) was prepared from 2-aminoethanol in 39% overall yield. 1,2-Di-O-palmitoyl-sn-glycero-3-phospho[alpha-(CH2)-H-2]choline (12) was prepared from N,N-dimethylglycine ethyl ester in 50% overall yield. (C) 1997 Elsevier Science Ireland Ltd.
Syntheses of 1,2-di-O-palmitoyl-sn-glycero-3-phosphocholine (DPPC) and analogs with 13C- and 2H-labeled choline head groups
摘要:
The syntheses of four head group labeled analogs of 1,2-di-O-palmitoyl-sn-glycero-3-phosphocholine (DPPC) (6) by a general method from 1,2-di-O-palmitoyl-sn-glycero-3-phosphatidic acid (5) have been performed. The syntheses of 1,2-di-O-palmitoyl-sn-glycero-3-phospho[alpha-C-13]choline (6a) and 1,2-di-O-palmitoyl-sn-glycero-3-phospho[beta-C-13]choline (6b) were performed from labeled [1-C-13]glycine (1a) in 52% overall yield and from [2-C-13]glycine (1b) in 56%, overall yield, respectively. 1,2-Di-O-palmitoyl-sn-glycero-3-phospho[N((CH3)-H-2)(3)]choline (9) was prepared from 2-aminoethanol in 39% overall yield. 1,2-Di-O-palmitoyl-sn-glycero-3-phospho[alpha-(CH2)-H-2]choline (12) was prepared from N,N-dimethylglycine ethyl ester in 50% overall yield. (C) 1997 Elsevier Science Ireland Ltd.
Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors
申请人:HALLEY Frank
公开号:US20090082379A1
公开(公告)日:2009-03-26
Compounds of formula (I):
wherein Ra, Rb, R, X
1
and X
2
are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.
N-methyl-2-dimethylaminoacetohydroxamic acid as a new reagent for the selective cleavage of active esters under neutral conditions
作者:Mitsunori Ono、Isamu Itoh
DOI:10.1016/s0040-4039(00)95161-x
日期:1989.1
A newreagent, N-methyl-2-dimethylaminoacetohydroxamic acid was developed for the selectivecleavage of active esters under neutral conditions. The kinetic studies and the applications of are described.
The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):
wherein R
1
is optionally substituted C1-C8 alkyl and the like; R
2
is C1-C6 alkyl; R
3
is C1-C6 alkyl and the like; or R
2
and R
3
taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R
4
is hydrogen and the like; G is a group selected from the groups shown by the formula an the like:
wherein R
5
is hydrogen and the like; X
1
is a single bond and the like; X
2
is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R
6
)—, wherein R
6
is hydrogen and the like, and the like; X
3
is a single bond and the like;
a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):
wherein R
1
, R
2
, R
3
, R
4
, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
申请人:Aventis Pharma S.A.
公开号:US07935819B2
公开(公告)日:2011-05-03
Compounds of formula (I):
wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.