Книга I: история любви 18
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| #4 ALEPH-2; 2,5-DIMETHOXY-4-ETHYLTHIOAMPHETAMINE SYNTHESIS: A solution of 2.0 g 2,5-dimethoxy-4-(ethylthio)benzaldehyde (see under 2C-T-2 for its synthesis) in 12 mL nitroethane was treated with 0.4 g anhydrous ammonium acetate and heated on the steam bath for 3 h. All volatiles were removed under vacuum, leaving a residue that set up as brilliant red crystals. These were mechanically removed from the evaporation flask, blown free of nitroethane vapor, and recrystallized from boiling EtOH, producing 1.8 g pale orange crystals, with a mp of 110-112 deg C. Recrystallization from 20 mL boiling IPA gave, after filtering and air drying, 1.70 g light orange crystals of 1-(2,5-dimethoxy-4-ethylthiophenyl)-2-nitropropene with a mp of 112-113 deg C. A suspension of 1.2 g LAH in 75 mL anhydrous THF was put under an inert atmosphere and, with good stirring, brought up to a gentle reflux. A solution of 1.5 g 1-(2,5-dimethoxy-4-ethylthiophenyl)-2-nitropropene in 20 mL anhydrous THF was added dropwise. Heating and stirring were maintained for an additional 24 h, and then the reaction mixture was allowed to come back to room temperature with stirring. There was added 1.4 mL H2O (dissolved in a little THF), followed by 1.4 mL 15% NaOH and finally another 4.2 mL H2O. Stirring was continued until all the curdy solids had turned white. The reaction mixture was filtered, and the filter cake washed with THF. The filtrate and the washings were combined, and the solvent removed under vacuum. The residue was 1.1 g of a pale amber oil. This was dissolved in 6 mL IPA, neutralized with concentrated HCl (about 8 drops were required) and then diluted with 150 mL anhydrous Et2O. The slightly cloudy solution was stirred for a couple of min, then there was the formation of a heavy white crystalline mass. This was removed by filtration, washed with Et2O, and air dried to provide 1.1 g 2,5-dimethoxy-4-ethylthioamphetamine hydrochloride (ALEPH-2) with a mp of 128-130 deg C with decomposition. DOSAGE: 4 - 8 mg DURATION: 8 - 16 h. QUALITATIVE COMMENTS: (with 4 mg) There was a warm feeling in the total body and a light pressure in the head that changed with time into the feeling of a balloon without any anatomical definition. The usual color perception was not very much increased, and my vision was not sharpened as it was with DOM. Rather, I noticed waves of movement, very smooth and not too busy. Both my tactile perception and auditory acuity were enhanced. The main effect for me was, paradoxically, an easier handling of the outer world. None of the jitters of amphetamine. The body feeling is good, healthy, and I am at peace with the body-mind dualism. These are pretty much personal comments Q I will write up the pharmacological points later. (with 5 mg) This turned out to be a day of extraordinary visuals and interpretations. About two hours into it, I felt that the effects were still climbing, but there was a marvelous onset of visual distortions and illusions, right at the edge of hallucination. The logs in the fireplace were in continuous motion. The notepaper I was writing on seemed to scrunch and deform under the pressure of the pen. Nothing would stay still; everything was always moving. There was a phase of unabated inflation. The intensity was noticeably dropping at the five hour point and I observed considerable residual shakes and a muscular tremor. Even towards midnight there was some tooth-rubbiness, but I was able to get a somewhat fretful though adequate sleep. (with 5 mg) I was exposed to a number of new environments and it was difficult to completely separate the experience into what was seen differently and what was seen for the first time. The Santa Cruz Mystery Spot should have been bizarre but it was simply hokey. And yet the boardwalk that should have been depressing was totally magical. The day was unworldly and I ended up with considerable muscular weakness. All in all, I handled it well, but I probably won't do it again. (with 7 mg) An amazing unification of visual hallucination seen only in the very fine detail of something, and what must be considered retinal hallucination. There is no one-to-one correspondence between the many retinal cells of the high-resolution part of the eye. Thus, the mind can pick and choose, sometimes from the right eye, and sometimes from the left. And so a small curve or bump can become whatever you wish. For a moment. And then it chooses again, but differently. Is all of our perceived world as subjective as this? (with 8 mg) Extreme intoxication, but almost no visual phenomena. Even well into the evening, I know I absolutely could not drive. Why? I don't know, since this experiment, at least, seemed to be quite free of strange colors and wiggly lines and streaks of light. It's that I don't trust that the reality I see is the same reality that the other driver might see. I am very much the center of the world about me, and I don't think I could trust anyone else to fully respect my reality. EXTENSIONS AND COMMENTARY: As with ALEPH itself, and in most ways with the entire ALEPH family, there is no predictability of the dose/response relationship. One person had expressed his psychic isolation by taking and maintaining a fetal position in relative hibernation for several hours and with substantial amnesia; this at a four milligram dose. Yet another person, at fully twice this amount, was aware of a slight light-headedness that could in no way be measured as more than a bare threshold. But by the time this erratic nature had become apparent, the ALEPHS had been assigned and made, up to and including ALEPH-7. ALEPH-3 was intended to be the methallylthio compound, 2,5-dimethoxy-4-(beta-methallylthio)amphetamine. The thioether (2,5-dimethoxyphenyl beta-methallyl sulfide) was easily made from 2,5-dimethoxythiophenol (see 2C-T-2 for its preparation) with 3.4 g dissolved in a solution of 1.7 g KOH in 25 mL boiling EtOH, and 2.72 g methallyl chloride, heated 1 h on the steam bath, poured into 250 mL H2O, extracted with 3x100 mL CH2Cl2, and solvent removal yielding 4.4 g of the sulfide as an amber oil. An effort to convert this to 2,5-dimethoxy-4-(beta-methallylthio)benzaldehyde (7.2 g POCl3, 6.7 g N-methylformanilide, 4.2 g of the crude sulfide from above, 15 min heating on the steam bath, H2O hydrolysis, hexane extraction of the residues from a CH2Cl2 extraction) produced 3.1 g of a peppermint-smelling oil that distilled at 140-160 deg C at 0.3 mm/Hg and which did indeed have an aldehyde group present (by proton NMR) but the rest of the spectrum was a mess, and the project was abandoned. Several years later, this entire project was reinitiated, and the aldehyde was obtained as a yellow crystal, but again it was not pursued. At that time, the earlier try had been totally forgotten, and a brand new ALEPH- (or 2C-T-) number had been assigned; i.e., 20. Thus, the corresponding phenethylamine (2,5-dimethoxy-4-(beta-methallylthio)phenethylamine), had it ever been made, which it was not, would have been called either 2C-T-3 or 2C-T-20, and the amphetamine homologue would probably have been ALEPH-20. A closely related 2C-T-X compound was also started quite a while later Q this was the allylthio homologue of the methallyl material 2C-T-3 or 2C-T-20. Its place in the flow of things is evident from its numbering, 2C-T-16. A mixture of 2,5-dimethoxythiophenol and KOH and allyl chloride in MeOH gave 2,5-dimethoxyphenyl allyl sulfide as a white oil which boiled at 110-125 deg C at 0.25 mm/Hg. This, with POCl3 and N-methylformanilide provided 2,5-dimethoxy-4-(allylthio)benzaldehyde which distilled at 140-160 deg C at 0.4 mm/Hg and could be recrystallized from MeOH as a pale yellow solid. Reaction of this aldehyde in nitroethane in the presence of ammonium acetate (steam bath for 2.5 h) provided 2,5-dimethoxy-4-allylthio-beta-nitrostyrene as red crystals from acetonitrile. Its mp was 114-115 deg C. Anal. (C13H15NO4S) C,H. This has not yet been reduced to the final amine, 2,5-dimethoxy-4-allylthiophenethylamine, 2C-T-16. The corresponding amphetamine would be, of course, ALEPH-16. ALEPH-5 was to be the cyclohexylthio analogue (2,5-dimethoxy-4-cyclohexylthioamphetamine). The thioether (2,5-dimethoxyphenyl cyclohexyl sulfide) was successfully made from 1.7 g 85% KOH pellets in 25 mL hot EtOH, 3.4 g 2,5-dimethoxythiophenol (again, see under 2C-T-2 for its preparation), and 4.9 g cyclohexyl bromide, 3 h on the steam bath, into 500 mL H2O, extraction with 3x100 mL CH2Cl2, washing the extracts with 5% NaOH, and evaporation to yield 5.2 g of an amber oil. The aldehyde, (made from 6.1 g POCl3 and 5.4 g N-methylformanilide, heated until claret colored, then treated with 5.0 g of the above crude thioether, heating for 20 min on the steam bath, into 300 mL H2O, and over-night stirring) was obtained as 3.1 g of a flesh-colored solid that was clearly neither pure nor completely correct. Repeated partitioning with organic solvents and cooling and scratching the residues finally provided a pale orange crystal (1.3 g, mp 88-93 deg C) which, after twice recrystallizing from MeOH, gave 0.4 g of pale yellow crystals with a mp 95-96 deg C and a textbook perfect NMR in CDCl3 (CHO, 1H (s) 10.41; ArH 2H (s) 6.93, 7.31; OCH3, 6H, (2s) at 3.88 and 3.92; CH, 1H br. at 3.34; and (CH2)5 10H br. at 1.20-2.34). The nitrostyrene was prepared from 200 mg of the above aldehyde in 1.2 mL nitroethane and 0.1 g ammonium acetate overnight on the steam bath, the solvent removed to give an orange oil that spontaneously crystallized after a few months' standing. This was never characterized, but sits there on the shelf to be reduced to ALEPH-5 some inspired day. The two-carbon homo-logue of this (2,5-dimethoxy-4-cyclohexylthiophenethylamine) will someday be called 2C-T-5 (if it is ever made). The remaining members of this family, ALEPH-4, ALEPH-6, and ALEPH-7 have actually been prepared and they have all been entered here in Book II, under their own names. #5 ALEPH-4; 2,5-DIMETHOXY-4-(i)-PROPYLTHIOAMPHETAMINE SYNTHESIS: A solution of 2.0 g 2,5-dimethoxy-4-((i)-propylthio)benzaldehyde (see under 2C-T-4 for its synthesis) in 12 mL nitroethane was treated with 0.4 g anhydrous ammonium acetate and heated on the steam bath for 12 h, then allowed to stir for another 12 h at room temperature. The excess solvent/reagent was removed under vacuum leaving a residue as a heavy deep orange two-phase oily mass. This was brought into one phase with 2 mL MeOH and then, with continued stirring, everything spontaneously crystallized. This product was removed by filtration and, after washing sparingly with cold MeOH and air drying, yielded 2.0 g of 1-(2,5-dimethoxy-4-(i)-propylthiophenyl)-2-nitropropene as orange crystals with a mp of 96-98 deg C. After recrystallization from 15 mL boiling 95% EtOH, filtering and air drying to constant weight, there was obtained 1.6 g of orange crystals with a mp of 99-100 deg C. A suspension of 1.0 g LAH in 100 mL warm THF was stirred under a N2 atmosphere and heated to a gentle reflux. To this there was added, dropwise, a solution of 1.2 g 1-(2,5-dimethoxy-4-(i)-propylthiophenyl)-2-nitropropene in 20 mL anhydrous THF. This mixture was held at reflux for 1 day, then stirred at room temperature for 2 days. There was then added, slowly and with caution, 1 mL of H2O, followed by 1 mL of 15% NaOH, and finally by another 3 mL of H2O. Stirring was continued until the reaction mixture became white and granular, then all solids were removed by filtration and the filter cake was washed with additional THF. The filtrate and washings were combined, and the solvent removed under vacuum to give 1.1 g of residue which was an almost white oil. This was dissolved in 6 mL IPA, neutralized with concentrated HCl (10 drops were required) and then diluted with 200 mL anhydrous Et2O. The resulting slightly turbid solution was clarified by filtration through a sintered glass filter, and the clear and slightly yellow filtrate was allowed to stand. A fine white crystalline product slowly separated over the next few h. This product, 2,5-dimethoxy-4-(i)-propylthioamphetamine hydrochloride (ALEPH-4) was removed by filtration, and after washing with Et2O and air drying, weighed 0.5 g and had a mp of 146-147 deg C, with prior sintering at 144 deg C. DOSAGE: 7 - 12 mg. DURATION: 12 - 20 h QUALITATIVE COMMENTS: (with 7 mg) Things started off going downhill, initially negative with tension and depression, but as the momentum developed, so did the positive effect. My discomfort continued to develop, but I was struck by the visual beauty of the trees and the small stream that flowed off the mountain. My experience continued to grow, simultaneously, in both the negative and the positive direction. Physically I was uncomfortable and found my breathing difficult, but I acknowledged a rapture in the very act of breathing. All moved over to the plus side with time, and the evening was gorgeous. I have never seen the sky so beautiful. The only flaw was when I choked on some lemonade and it seemed to me I almost drowned. I have been extremely conscious of eating, drinking and swallowing ever since. I barely slept the whole night and awoke extremely tired. I felt that the experience continued for many days, and I feel that it is one of the most profound and deep learning experiences I have had. I will try it again, but will block out more time for it. (with 8 mg) There was without question a plus two, but none of the edges of unreality that are part of LSD. The sounds that are just outside of my hearing are intriguing, and distract me from the eyes-closed imagery that is just barely possible with music while lying down. But, going outside, there were no obvious sources of the sounds that I heard. Could I drive? I suspect so. I took a shower and did just that Q I drove to San Francisco without incident, and walked amongst the many strange faces on the downtown streets. (with 12 mg) The experience was very intense but completely under control except for a twenty minute period right in the middle of it. I had to get away from everything, from everyone. There was a sense of being surrounded and moved in upon that was suffocating. I was weighed down with everything Q physical, psychic, emotional. My clothes had to come off, my hair had to be released, my shoes went, I needed to move away from where I was, to somewhere else, to some new place, any new place, with the hope that my other old place wouldn't follow me. Pretty soon I found I was myself, I could breathe again, and I was OK. Rather sheepishly, I dressed and rejoined the group. The rest of the day was spectacular, but those few minutes were scary. What if I couldn't have escaped? EXTENSIONS AND COMMENTARY: Again, there are hints and suggestions of complexities. These, and several other reports, suggest some sensory confusion, and interpretive aspects that are to some extent threatening. There is an underlying suggestion of body toxicity. I know of no experiment that exceeded 12 milligrams and I would not be able to predict what might come forth at higher dosages. I personally choose not to try them. |
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